MEDIWednesday, 13 September 2006

7:00 PM-9:00 PM Moscone Center -- Hall D, Poster
General Poster Session
Sponsored by Nature Reviews Drug Discovery
Organizer:David P. Rotella
Chemoenzymatic synthesis of (R)-Nifenalol via yeast-mediated symmetric reduction of ketones
Jian-He Xu, Wei Yang
De Novo design and synthesis of novel RNA polymerase inhibitors as potential anti-tuberculosis agents
Anil K. Agarwal, Julian G. Hurdle, Amer I. AlOmar, Ian Chopra, A Peter Johnson, Colin W. G. Fishwick
Pyrrolidine carboxamide as novel class inhibitor of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis (InhA)
Xin He, Alian Akram, Robert Stroud, Paul R. Ortiz de Montellano
Benzothienoquinolines, N-10 bioisosteres of cryptolepine as novel antiifectives with lower cytotoxicity
Seth Y. Ablordeppey, Xue Y. Zhu, Melissa Jacob, Shabana I. Khan, Larry A. Walker
Phenylimidazole and 4-pyridone hybrid derivatives as novel inhibitors of bacterial enoyl-ACP reductases FabI and FabK
Hideo Kitagawa, Tomohiro Ozawa, Sho Takahata, Maiko Iida, Jun Saito, Takashi Watanabe, Eiki Shitara
Application of regioselective Staudinger reaction: Expedient synthesis and antibacterial evaluation of novel aminoglycoside antibiotics related to butirosin and amikacin
Jie Li, Hsiao-Nung Chen, Cheng-Wei T. Chang
Studies towards synthesis and medicinal applications of antibiotic Ficellomycin
Gang Chen, Andrei K Yudin
Discovery and SAR of diphenylborinic acid picolinate esters as a potent antibacterial and anti-inflammatory agent for the treatment of skin diseases
Tsutomu Akama, Stephen J. Baker, Yong-Kang Zhang, Vittorio Sauro, Rajeshwar Singh, Kirk Maples, Jacob J. Plattner, Stephen J. Benkovic, Ving Lee
Optimization of pharmacokinetic properties of pyrazolopyrimidinediones, selective inhibitors of Helicobacter pylori
Pamela J. Hill, Gregory S. Basarab, Abdullah Rastagar, Peter Webborn
Synthesis and biological activity study of potent inhibitors against aminoglycoside N-6' acetyltransferase: An important antibiotic resistance enzyme
Feng Gao, Xuxu Yan, Karine Auclair
CYP3A4 inhibitory studies on a new series of macrolides
Dahua Pan, Wenzhong Liang, Zhaohai Zhu, Scott G. Franzblau
2,6-Hexadecadiynoic acid and 2,6-nonadecadiynoic acid: Novel synthesized acetylenic fatty acids as potent antifungal agents
Néstor M. Carballeira, David Sanabria, Keykavous Parang
Antibacterial agents from multivalent design of antimicrobial peptides and combinatorial library screening
Zhigang Liu, Chunhui Zhou, Anne Young, Heather Deshazer, Amanda Rice, Neville R Kallenbach
Surfactant-free nanoparticles for delivering antibiotics
Julio Cesar Garay, Kerriann Robyn Greenhalgh, Edward Turos
Novel polyacrylamide nanoparticles for delivery of N-thiolated β-lactam antibiotics
Yang Helen Wang, Kerriann Robyn Greenhalgh, Edward Turos
Heterosubstituted N-thiolated beta lactam antibiotics
Praveen Ramaraju, Timothy E. Long, Edward Turos
1,2-Dioxolanes as carbon isosteres of antimalarial 1,2,4-trioxolanes: Effects on chemical stability and antimalarial activity
Xiaofang Wang, Yuxiang Dong, Sergio Wittlin, Jonathan L. Vennerstrom
Peterson olefination tool for synthesis of three new azasterols. Possible inhibitors of the Delta-(24,25) sterol methyl transferase
Gonzalo G Visbal, Luis Corredor
Formation of primary and secondary carbon-centered radicals in the iron (II)-mediated decomposition of antimalarial 1,2,4,5-tetraoxanes
Yuxiang Dong, Jonathan L. Vennerstrom
Structure-based design and synthesis of conformationally constrained inhibitors of parasitic cysteine proteases
Yen Ting Chen, Ricardo Lira, Jason J. Reddick, Elizabeth Hansell, James H. McKerrow, William R. Roush
Peptidyl vinyl sulfonyl inhibitors of cysteine protease: Development and biologically activity
Michael H. Ober, Yen Ting Chen, Elizabeth Hansell, James H. McKerrow, William R. Roush
Investigation of the antimicrobial properties of polycationic carbohydrate derivatives
Marie Thomas, Alejandra Castano, Laura Friedman, Heidi Lee, Jay Leb, Leah Rothman, Karin Melkonian, Robert Engel
Phosphoramidate pronucleotides: A comparison of the phosphoramidase substrate specificity of human and E. coli histidine triad nucleotide binding proteins (hint)
Tsui-Fen Chou, Janina Baraniak, Xin Zhou, Carston R. Wagner
Synthesis and evaluation of novel bisphosphonates targeting Undecaprenyl diphosphate synthase
Rong Cao, Yonghui Zhang, Fenglin Yin, Michael Hudock, Rey-ting Guo, Andrew H-J. Wang, Eric Oldfield
Activity of 6-O-substituted macrolides against Mycobacterium tuberculosis
Zhaohai Zhu, Valentina Z. Petukhova, Dahua Pan, Baojie Wan, Yuehong Wang, Olga Krasnykh, Gengli Yu, Kate Schellinger, Scott G. Franzblau
Bypassing antibiotic resistance: Development of novel pronucleotides as antibacterials
Mallinath B. Hadimani, Andrew M. Lee, Scott F Singleton
Synthesis of phosphorous-containing folate and methotrexate analogs as potential inhibitors of dihydrofolate synthetase and antimalarial drugs
Yonghong Yang, James K. Coward
Design, synthesis and broad antiparasitic activity of potent triclabendazole-sulfoxide bioisosteres
Gabriel Navarrete-Vazquez, Alicia Hernandez-Campos, Francisco Hernandez-Luis, Lilián Yépez-Mulia, Rafael Castillo
Synthesis and antiamoebic activity of new ferrocene-metronidazole analogs against Entamoeba histolytica
Shailendra Singh, Neelam Bharti, Amir Azam
Evaluation of metal-chloroquine derivatives in the inhibition of β-Hematin formation
Maribel Navarro, William Castro
Discovery of high affinity peptide ligand for Vancomycin
Nianhuan Yao, Kit S. Lam
Probing the structures of leishmanial farnesyl pyrophosphate synthases: Homology modeling and docking studies
Prasenjit Mukherjee, Prashant V. Desai, Anuradha Srivastava, Mitchell A. Avery, Babu L. Tekwani
Synthesis and antiprotozoal activity of methyl (1-methyl-1H-benzimidazol-2-yl)carbamate derivatives
Rafael Castillo, Antonio Hernández, Francisco Hernandez-Luis, Lilián Yépez-Mulia, Fernanda Frausto-Castorena, Alicia Hernandez-Campos
Paper Withdrawn
Sulfonamide hydroxamic acid anthrax lethal factor inhibitors: Improved selectivity over MMPs
Seongjin Kim, Christopher Bayne, Melissa Nagata, Minda Yamaga, Lynne Cregar, Linda McKasson, Sean O'Malley, Sherri Mills, Mark Goldman, Cho Tang
Inhibitors of tryptophanyl-tRNA synthetase from Plasmodium falciparum via in situ click chemistry
Suresh M. Pitram, Zhanna Druzina, Valery V. Fokin, Paul Schimmel, K. Barry Sharpless
Synthesis and antiprotozoal activity of nitrothiazole-benzimidazole hybrid carboxamides
Olivia Soria-Arteche, Alicia Hernandez-Campos, Francisco Hernandez-Luis, Ivone Rosas-Martínez, Lilián Yépez-Mulia, Rafael Castillo
Synthesis and SAR for linker in tethered dimer inhibitors of NAD synthetase
Wayne J. Brouillette, Liyuan Mou, Christie G. Brouillette, Chi-Hao Luan, Lawrence J. DeLucas
Design and synthesis of a novel nanomolar inhibitor of Toxoplasma gondii dihydrofolate reductase, its salt form and analogs
Aleem Gangjee, Xin Lin, Lisa R. Biondo, Sherry F. Queener
Investigating the interaction between protozoan DNA-binding protein, JBP-1 and glycosylated DNA
Rajesh K. Grover, Stephanie J. Pond, Mariceli Puga, Prem S. Subramaniam, Charles Weissmann, Piet Borst, David P. Millar, Paul Wentworth Jr.
Drug discovery targeted the GHKL superfamily
Xinshan Kang, Boris Klebansky, Richard Fine
Synthesis and SAR studies of potent imidazopyridine anticoccidial agents
Xiaoxia Qian, Gui-Bai Liang, Danqing D. Feng, Michael H. Fisher, Chris Brown, Anne Gurnett, Penny Leavitt, Paul Liberator, Andrew Misura, Samantha Samaras, Tamas Tamas, Dennis M. Schamtz, M. J. Wyvratt, Tesfaye Biftu
Molecular modeling of some 1H-benzimidazole derivatives with antiamoebic activity: A comparative molecular field analysis study
Fabian López-Vallejo, José Luis Medina-Franco, Sergio Rodríguez-Morales, Alicia Hernández-Campos, Francisco Hernández-Luis, Lilián Yépez-Mulia, Rafael Castillo
Systematic investigation of the effect of sidechain basicity and length on the antimalarial activity of 7-chloroquinolines
Kimberly S. Yearick, John N. Alumasa, Jayakumar K. Natarajan, Paul Roepe, Christian Wolf
pH-dependent metal ion binding studies on Dapson
Hadijatu Mumini, Nsoki Phambu, Baibai Kamara
Development of new anti-malarial drugs derived from chloroquine
Kekeli Ekoue-kovi, John, N Alumasa, Jayakumar K. Natarajan, Paul D. Roepe, Christian Wolf, Kimberly, S Yearick
Synthesis and evaluation of mechanism-based inhibitors of plasmepsin II
Deepak Gupta, Patrick M. Woster
Structure-activity relationships for a series of inhibitors of purine nucleoside phosphorylase from Schistosoma mansoni
Adriano D. Andricopulo, Glaucius Oliva, Marcelo S. Castilho, Marcela F. Terni, Richard C. Garratt, Matheus P. Postigo
Potent and orally active GSK-3 inhibitors
Leyi Gong, Claudia Tan, Don Hirschfeld, Heather Hogg, Gary Peltz, Andrew Grupe, Zafrira Avnur, Pete Dunten
Discovery of selective JNK1 inhibitors
Hanna Cho, Songyuan Shi, Shumeye Mamo, Wayne Spevak, Shenghua Shi, Hu Pan, Abhinav Kumar, Billy Lam, Brian West, Catherine Luu, Chao Zhang, Daniel Fong, Gaston Habits, Gideon Bollag, John Cantwell, Julie Rice, Kam Zhang, Kevin Eng, Rafe Shellooe, Rick Artis, Yong-Liang Zhu, Yoshihisa Suzuki, Prabha Ibrahim
Structure-activity relationship of sterol mimetic (1) analogs: Potent LXR agonists to upregulate ABCA1 gene expression
Robert H. Jiang, Matthew M. Abelman, Bindu Joshi, Jeffrey Chisholm, Jia Hao, Nancy Chu, Nevena Mollova, Kwan Leung, Jeff A. Zablocki
Towards the design, synthesis and evaluation of novel RAR ligands
Shyam Desai, Weilin Sun, Zhenping Zhang, Jerome L. Gabriel, Dianne Soprano, Daniel J. Canney
Indanylacetic acids carrying 4-thiazolyl/oxazolyl-phenyl tail groups, a new class of balanced PPAR alpha/gamma/delta triple agonists: Synthesis, SAR and in vivo efficacy
Joachim Rudolph, Libing Chen, Dyuti Majumdar, William H. Bullock, Michael Burns, Soongyu Choi, Thomas Claus, Fernando E. Dela Cruz, Michelle Daly, Frederick J. Ehrgott, Jeffrey S. Johnson, James N. Livingston, Michelle Nophsker, Robert W. Schoenleber, Jeffrey Shapiro, Susan Tomlinson, Christopher Town, Ling Yang, Manami Tsutsumi, Xin Ma
Indanylacetic acid derivatives carrying aryl-pyridyl and aryl-pyrimidinyl tail groups: A new class of PPAR gamma/delta and PPAR alpha/gamma/delta agonists
Louis-David Cantin, Sidney Liang, Herbert Ogutu, Christiana I. Iwuagwu, William H. Bullock, Michael Burns, Roger Clark, Thomas Claus, Fernando E. dela Cruz, Michelle Daly, Frederick J. Ehrgott, Jeffrey S. Johnson, James N. Livingston, Michelle Nophsker, Robert W. Schoenleber, Jeffrey Shapiro, Christopher Town, Ling Yang, Manami Tsutsumi, Xin Ma
Indole acetic acid derivatives incorporating [(thiazolyl/oxazolyl)-phenoxy/pyridyloxy] tail groups – novel, potent PPAR alpha/gamma/delta triple agonists: Synthesis, SAR, and in vivo efficacy
Xin Ma, Martin Hentemann, Joachim Rudolph, William H. Bullock, Michael Burns, Louis-David Cantin, Libing Chen, Soongyu Choi, Roger Clark, Thomas Claus, Fernando E. Dela Cruz, Michelle Daly, Frederick J. Ehrgott, Christiana I. Iwuagwu, Jeffrey S. Johnson, Ellalahewage Kumarasinghe, Rico Lavoie, Sidney Liang, James N. Livingston, Dyuti Majumdar, Michelle Nophsker, Herbert Ogutu, Robert W. Schoenleber, Jeffrey Shapiro, Kanwar Sidhu, Christopher Town, Susan Tomlinson, Philip L. Wickens, Ling Yang, Zhonghua Zhang, Manami Tsutsumi
Sulfonylureas as partial PPAR gamma agonists
Hiroo Koyama, Daniel J. Miller, Peter T. Meinke, Joel P. Berger, Thomas W. Doebber, David E. Moller, Soumya P. Sahoo
Design, synthesis and biological evaluation of novel PPAR a/g dual agonists
Nam-Jung Kim, Seung-Mann Paek, Hwa-Young Yun, Bon Woong Koo, Youn-Hee Nam, Young-Ger Suh
Design and synthesis of 3-{4-[3-(2-aryl-2-yl-phenoxy)butoxy]-phenyl}propionic acids: A new class of dual PPAR&gamma/&delta agonists
Isabel C. Gonzalez, Jason Lamar, Fatima Iradier, Yanping Xu, Leonard Winneroski, Jeremy York, Nathan Yumibe, Richard Zink, Chahrzad Montrose-Rafizadeh, Gary Etgen, Carolyn Broderick, Brian Oldham, Nathan B. Mantlo
Design and synthesis of novel and potent amide linked PPAR gamma/delta dual agonists
Qing Shi, Emily J. Canada, Yanping Xu, Garret J. Etgen, Alan Warshawsky, Carol L. Broderick, Cathleen K. Clutinger, Lynnie A. Irwin, Michael E. Laurila, Chahrzad Montrose-Rafizadeh, Brian A. Oldham, Minmin Wang, Leonard L. Winneroski, Chaoyu Xie, Jeremy S. York, Nathan P. Yumibe, Richard W. Zink, Nathan B. Mantlo
Identification of highly potent and subtype-selective PPARalpha agonists as efficacious lipid modulating agents
Guo Q. Shi, Yong Zhang, James F. Dropinslki, Soumya P. Sahoo, Jeol P. Berger, Taro E. Akiyama, Gaochao Zhou, Raul Alvaro, Tian-quan Cai, Peter T. Meinke
Toward PPAR agonists as novel therapeutics for inflammation and CNS disorders
Upasana Mehra, Jack J. Lin, Gaston Habets, Prabha N. Ibrahim, Rick Artis, Chao Zhang
Synthesis and LXR activity of 3-[substituted phenyl] quinolines
John W. Ullrich, Robert L. Morris, Ronald C. Bernotas, David Kaufman, Ponnal Nambi, Elaine Quinet, Liang Chen, Anita Halpern, Qiang-Yuan Liu, Dawn Savio, Mike Basso, Ray J Unwalla, Anna Wilhelmsson, Annika Goos Nilsson, Crina Ursu, Erik Arnelof, Johnny Sandberg, Christopher Enroth, Jay Wrobel
Exploration of the S4 binding element in amino acid-derived fXa inhibitors via parallel synthesis
Jothirajah Marimuthu, Nickolay Y Chirgadze, Trelia J. Craft, Ronald S Foster, Jeffry B. Franciskovich, Larry L. Froelich, Peter R. Guzzo, Valentine J. Klimkowski, Jeffery K. Kyle, Michael J. Mayer, Donetta S. Gifford-Moore, Christopher W. Murray, John W. Liebeschuetz, John J. Masters, Jeffrey K. Smallwood, Gerald F. Smith, Sarah M. Smith, Richard D. Towner, Stephen C. Young, Michael R. Wiley
Synthesis of potent, selective and neutral inhibitors of FXa
Ulf E. Fahlander, Kenneth L. Granberg, Emma Bratt, Kristina Nilsson, Jens Petersen, Yantao Chen, Ingemar Nilsson, Leifeng Cheng, Kosrat Amin, Kevin Foote, John W Rayner, Johan Broddefalk, Saswati Ghosal, Björn Holm, Johan Sundell, Johanna Deinum, Margareta Elg, Daniel Hovdal
Paper Withdrawn
Unusual alkylation of pyridazinone in FXa inhibitors
Emma Bratt, Kenneth L. Granberg, Johanna Deinum
Optimization of piperazinone derivatives as FXa inhibitors
Kenneth L. Granberg, Emma Bratt, Ulf E. Fahlander, Ingemar Nilsson, Kosrat Amin, Björn Holm, Huascar Villanueva, Christer Alstermark, Jens Petersen, Johanna Deinum, Margareta Elg, Ann-Charlotte Egnell, Daniel Hovdal
Balancing properties of FXa inhibitors
Ulf E. Fahlander, Kenneth L. Granberg, Kosrat Amin, Emma Bratt, Christer Alstermark, Jens Petersen, Ingemar Nilsson, Kristina Nilsson, Fredrik Zetterberg, Saswati Ghosal, Björn Holm, Johan Broddefalk, Leifeng Cheng, Kevin Foote, John W Rayner, Johanna Deinum, Margareta Elg, Daniel Hovdal, Ann-Charlotte Egnell
Synthesis and SAR of 1,2-cis cyclic diamide-based inhibitors of coagulation factor Xa
Jennifer X. Qiao, Tammy Wang, Sarah R. King, Gren Z Wang, Changhwan Chang, Daniel L. Cheney, Alan Rendina, Kan He, Joseph M. Luettgen, Robert M. Knabb, Ruth Wexler, Patrick Y. S. Lam
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties
James R. Corte, Tianan Fang, Donald J. P. Pinto, Wei Han, Zilun Hu, Xiang-Jun Jiang, Yun-Long Li, Alan R. Rendina, Joseph M. Luettgen, Pancras C. Wong, Kan He, Chong-Hwan Chang, Daniel L. Cheney, Robert M. Knabb, Ruth R. Wexler, Patrick Y. S. Lam, Jolicia F. Gauuan, Mark Hadden, Darren Orton
Aminomethyl pyrrolidine as a novel scaffold for FXa inhibitors
Yan Shi, Jing Zhang, Philip D. Stein, Ying Wang, Lawrence J. Kennedy, Stephen P. O'Connor, Saleem Ahmad, Wei Han, Zilun Hu, Doree Sitkoff, Patrick Y. S. Lam, Karnail Atwal, Jeff A. Robl, Eddie C-K. Liu, Karen S. Hartl, Steven M. Seiler, Ruth R. Wexler, Robert Zahler
Synthesis of muraglitazar 12-carboxylic acid metabolite
Yande Huang, Donglu Zhang, Venkatapuram Palaniswamy
3-Phosphinoylpropionic acid inhibitors of Thrombin Activatable Fibrinolysis Inhibitor (TAFI) 1: Design, synthesis and biological activity
Kumar Emayan, Shendong Yuan, Imadul Islam, Paul M. Hrvatin, Christopher West, Zheng Chang, Judi Bryant, Kieu Chu, Drew Sukovich, Brad O. Buckman
3-Phosphinoylpropionic acid inhibitors of Thrombin Activatable Fibrinolysis Inhibitor (TAFI) 2: In vitro and in vivo evaluation
Shendong Yuan, Kumar Emayan, Imadul Islam, Paul M. Hrvatin, Christopher West, Zheng Chang, Judi Bryant, Kieu Chu, Drew Sukovich, John Morser, Bill Dole, Mariko Nagashima, Ron Vergona, Kathy White, Jim Wang, Valdeci DaCunha, John Vincelette, Kohichi Kawai, Lei Zhao, Brad O. Buckman
3-Phosphinoylpropionic acid inhibitors of Thrombin Activatable Fibrinolysis Inhibitor (TAFI) 3: Crystal structure of 3-phosphinoylpropionic acid inhibitors bound to carboxypeptidase B
Marc Adler, Marc Whitlow, Shendong Yuan, Kumar Emayan, Imadul Islam, Paul M. Hrvatin, Christopher West, Zheng Chang, Judi Bryant, Brent Larson, Brad O. Buckman
Hit to lead discovery of potent 11b-HSD1 inhibitors
Ravi Kurukulasuriya, Vince S. C. Yeh, William J. Chiou, Steven Fung, Jiahong Wang, Hing L. Sham, James T. Link
Discovery of anilinothiazolone analogs as 11beta-HSD1 inhibitors
Chester Yuan, David J. St. Jean Jr., Qingyian Liu, Lynn Cai, Aiwen Li, Nianhe Han, Ben Askew, Randall Hungate, Lars Johansson, Lars Tedenborg, David Pyring, Meredith Williams, Minghan Wang, Clarence Hale, Jiandong Zhang, Steven Jordan, Michael Bartberger, Yaxiong Sun, Maurice Emery, Christopher H. Fotsch
Discovery of potent and selective 11ß-HSD-1 inhibitors
Jyoti R. Patel, Qi Shuai, Jurgen Dinges, Martin Winn, Marina Pliushchev, Steven Fung, Katina Monzon, Jiahong Wang, William J. Chiou, Liping Pan, Kenton Longenecker, Hing L. Sham, Peer Jacobson, J. T. Link
Discovery and SAR of novel 11ß-hydroxysteroid dehydrogenase type I inhibitors
Qi Shuai, Jyoti R. Patel, Jeffrey J. Rohde, Marina Pliushchev, Jurgen Dinges, Steven Fung, Katina Monzon, Jiahong Wang, Liping Pan, Hing L. Sham, Peer Jacobson, J. T. Link
SAR studies on a novel series of potent ACC2 inhibitors for treatment of obesity and type 2 diabetes
Tianyuan Zhang, Richard F. Clark, Todd M. Hansen, Zhili Xin, Gang Liu, Xiaojun Wang, Rongqi Wang, Heidi S. Camp, Bruce A. Beutel, Hing L. Sham, Yu Gui Gu
Tetrahydroquinolines as novel cannabinoid-1 receptor antagonists
Chongqing Sun, Doree Sitkoff, Yanting Huang, Yan Zhou, Zhengxiang Gu, Natesan Murugesan, Liya Kang, Yifan Yang, RoseAnn Baska, Mary Jane Cullen, MaryAnn Pelleymounter, Paul Stetsko, Olafur Gudmunsson, Oliver Flint, Susan Johngher, Steven Wu, Kamelia Behnia, Kenneth Carlson, William R. Ewing
Design, SAR and in vivo evaluation of 5-HT2C receptor agonists for the treatment of obesity
Dean A. Wacker, Jeffrey G. Varnes, Keith J. Miller, Thao Ung, Ginger Wu, Chen-Pin Hung, Sarah Malmstrom, Ge Zhang, Eva Otanyi, William J. Keim, Mary Jane Cullen, Kenneth W. Rohrbach, Qu Qinling, Rangaraj Narayanan, Karen Rossi, Mary Ann Pelleymounter, Jeffrey A. Robl
Design and synthesis of potent and selective 5-HT2c receptor agonists
Guohua Zhao, Chet Y. Kwon, Sharon N. Bisaha, Philip D. Stein, Chen-Pin Hung, Ginger Wu, Thao Ung, Xueying Cao, Keith J. Miller, Sarah Malmstrom, Ge Zhang, Eva Otanyi, William J. Keim, Mary Jane Cullen, Kenneth W. Rohrbach, Jinping Gan, Mary Ann Pelleymounter, Jeffrey A. Robl
Synthesis and biological evaluation of dihydroquinazolinones as potent and selective 5-HT2C receptor agonists
Saleem Ahmad, Khehyong Ngu, Keith Miller, Ginger Wu, Chen-pin Hung, Sarah Malmstrom, Ge Zhang, Eva Otanyi, William J. Keim, Mary Jane Cullen, Kenneth W. Rohrbach, Michael Thomas, Jinping Gan, Rangaraj Narayanan, Mary Ann Pelleymounter, Jeffrey Robl
The synthesis and SAR of MC4R agonists for the treatment of obesity
Iyassu K. Sebhat, Yingjie Lai, Khaled Barakat, Rui Tang, Rubana N. Kalyani, Aurawan Vongs, Tanya MacNeil, David H. Weinberg, Tung M. Fong, Lex Van der Ploeg, Arthur A. Patchett, Matthew J. Wyvratt, Ravi P. Nargund
Microwave assisted synthesis of thiazolo-, isothiazolo-, imidazolo-, and pyrimido-pyrimidinones as novel MCH1R antagonists
Rui Zhang, Rachael C. Hunter, Tao Guo
Design and synthesis of orally efficacious piperidine-based melanin-concentrating hormone receptor 1 antagonists
Wen-Lian Wu, Duane A Burnett, Mary Ann Caplen, Martin S Domalski, Chad Bennett, Richard Spring, Li Qiang, Thavalakulamgara K Sasikumar, William J Greenlee, Brian E Hawes, Kim O'Neill, Blair Weig, Brian Spar, Daniel Weston, Timothy Kowalski
Regioisomeric bicyclo[3.1.0]hexyl urea MCH-R1 antagonists: Addressing the fragmentation issues of bicyclohexyl ureas
Mark D. McBriar, Ruo Xu, John W. Clader, Brian E. Hawes, Kim O'Neill, Daniel Weston, Kathleen Cox
MCH receptor-1 antagonists for the treatment of obesity
Anthony L Handlon, Kamal A Al-Barazanji, Kevin K Barvian, Andrew J Carpenter, Joel P Cooper, Aaron S Goetz, Gary M Green, Yu C Guo, Donald L Hertzog, Clifton E Hyman, Gregory E Peckham, Jason D Speake, Francis X Tavares, Hui-qiang Zhou
Novel cyclic lactam α-MSH analogs as potent and selective hMC3R agonists and antagonists, and hMC1R antagonists
Alexander V. Mayorov, Minying Cai, So-Yeop Han, Bahar Tan, April R. Van Scoy, Matthew Dedek, Erin S. Palmer, Dev Trivedi, Victor J. Hruby
Cyclopropylglycine amide derivatives as potent DPP-IV inhibitors for the treatment of diabetes
Abraham Thomas, Ashok Kadam, Mangesh Pawar, Daisy Shah, Kanthikiran Varanasi, Anupindi Raghuram, Shridhar Narayanan, Swaroop V. Vakkalanka
3-[2-((2S)-2-Cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogs as DPP-IV inhibitors for the treatment of type-II diabetes
Hsing-Pang Hsieh, Mohane S. Coumar, Chung-Nien chang, Ssu-Hui Wu, Xin Chen, Chiung-Tong Chen, Weir-Torn Jiaang
Synthesis and the structure-activity relationships of cyclohexene-constrained phyenethylamine as Dipeptidyl Peptidase IV inhibitor
Xiaofeng Li, Zhonghua Pei, Thomas W. von Geldern, David J. Madar, Kenton Longenecker, Hong Yong, Thomas H. Lubben, Kent D. Stewart, Stephen J. Ballaron, Michael A. Stashko, Amanda K. Mika, David W. A. Beno, Glenn A. Reinhart, Anita J. Kempf-Grote, Hing L. Sham, James M. Trevillyan
Potent inhibitors of DPP-IV: 2-cyano-4-fluoro-1-thiovalylpyrrolidine analogs
Steven M. Reister, Curt D. Haffner, Darryl L. McDougald, Brian D. Thompson, Christopher Conlee, Jing Fang, Jonathan Bass, James M. Lenhard, Dallas Croom, Melissa B. Secosky-Chang, Thaddeus Tomaszek, Donovan McConn, Kevin Wells-Knecht, Paul R. Johnson
Discovery of indazole derivatives as potent leukotriene A4 hydrolase inhibitors
Lei Zhao, Bjorn Mamat, Rama Mishra, Guđrún Halldórsdóttir, Heioa Sigporsdottir, Thorkell Andression, David Zembower, Mark Gurney, Jasbir Singh, Vincent Sandanayaka
Design, synthesis, and SAR of novel leukotriene A4 hydrolase inhibitors containing chiral piperidine and piperazine scaffolds
Vincent Sandanayaka, Bjorn Mamat, Louis Bedell, Nikhil Bhagat, Brian Bock, Michael Krohn, Rama Mishra, Emmanuel Onua, Jun Zhang, Guđrún Halldórsdóttir, Heiđa Sigţórsdóttir, Thorkell Andression, David Zembower, Mark Gurney, Jasbir Singh
Azabenzimidazole-aminofurazans as potent and selective Rho-kinase inhibitors
Robert A. Stavenger, Dennis Lee, Robert L. Ivy, Weiwei Xu, Simon F. Semus, Larry J. Jolivette, Lois L. Wright, Ross Bentley, Christopher P. Doe, Erding Hu
Potent ABCA1 elevating compounds, derivatives of tranexamic acid
Dmitry Koltun, Melanie Boze, Bindu Joshi, Richard Lawn, Jia Hao, David Lustig, Kwan Leung, Jeff Zablocki
Tetrahydro napthyridine as inhibitors of cholesteryl ester transfer protein
Saravanan Parthasarathy, Maria-Carmen Fernandez, Ana I Mateo, Ana Escribano, Eva M Martin de la Nava, Xiaodong Wang, Sandra L Cockerham, Thomas P Beyer, Robert J Schmidt, Guoging Cao, Gregory Stephenson, Nathan B Mantlo
Potent, macrocyclic motilin receptor antagonists incorporating new unnatural amino acids
Eric Marsault, Kamel Benakli, Sylvie Beaubien, Carl Saint-Louis, Robert Déziel, Graeme Fraser
Potent and selective protein tyrosine phosphatase 1b inhibitors
Zhao-Kui Wan, Jinbo Lee, Douglas Wilson, Dave Erbe, Weixin Xu, Yan-Ling Zhang, Lori Klaman, Diane Joseph-McCarthy, Xin Xu, Bruce Follows, Junjun Wu, Steven Kirincich, Alessandro F. Moretto, Eva Binnun, Rajeev Hotchandani, Manus Ipek, May Tam, Sarah Will, Ariful Qadri, James Tobin, Steve Tam
Probing acid replacements of PTP1B inhibitors
Steven J. Kirincich, Bruce Follows, Zhao-Kui Wan, Douglas P. Wilson, Junjun Wu, Weixin Xu, Diane Joseph-McCarthy, May Tam, Dave Erbe, Steve Tam, James Tobin, Yanling Zhang, Jinbo Lee
Polycyclic thiophenes as protein tyrosine phosphatase 1B inhibitors
Alessandro F. Moretto, Steven J. Kirincich, WX. Xu, Michael J. Smith, Zhao-Kui Wan, Douglas P. Wilson, Bruce Follows, Eva Binnun, Diane Joseph-McCarthy, Kenneth Foreman, Dave Erbe, Yanling Zhang, Steve Tam, Jinbo Lee
P2Y1 antagonists: An analysis of the structural elements of ligand recognition based on molecular docking and 3D-QSAR
Stefano Costanzi, Michihiro Ohno, Eun Joo Roh, Bhalchandra V. Joshi, Anny-Odile Colson, Dayle Houston, Savitri Maddileti, T. Kendall Harden, Kenneth Jacobson
Selective benzimidazolone ß3 adrenergic receptor agonists with reduced rat atrial tachycardia
Don R. Finley, William E. Bloomquist, Donald B. Bennett, Marlene L. Cohen, Mark L. Heiman, Aidas Kriauciunas, Daniel J. Sall, Frank C. Tinsley, Cynthia D Jesudason
Synthesis and SAR of novel alkoxyphenyl pyrazole urea derivatives
Honnappa Jayakumar, Bradley R. Teegarden, Sonja Strah-Pleynet, Hongmei Li, Naomi Kato, Katie Elwell, Susan D. Selaya, Karen Chang, Jarrod Davidson, Jonathan Foster, Stephan Espitia, Hazel Reyes, Xiaohua Chen, William Thomsen
Synthesis and SAR of solubilized pyrazole derivatives as 5HT2A inverse-agonists for platelet aggregation
Peter Dosa, Bradley Teegarden, Honnappa Jayakumar, Sonja Strah-Pleynet, Yifeng Xiong, Martin Casper, Jin Sun Choi, Marc Decaire, Hongmei Li, Katie Elwell, John Adams, Stephen Espitia, Juan Ramirez, Jeremy Richman, William Thomsen, Diane Yuskin, Hong Zheng
Design and synthesis of 2-amino-4-anilino-6-substituted pyrrolo[2,3-d]pyrimidines as antiangiogenic agents
Aleem Gangjee, Ojas A. Namjoshi, Michael Ihnat, Linda A. Warnke, Jessica E. Thorpe
The efficient synthesis for the segment of Aliskiren
Rujian Ma, Feiyu Tang, Shuhui Chen, Ge Li
Selective PDE11A inhibitors as glucose-dependent insulin secretagogues: Synthesis and SAR of 1,8-naphthyridinones
Yamin Wang, Teresa Bear, William Bullock, Libing Chen, Leatte Guernon, David Gunn, Laszlo Hunyadi, Richard Kramss, Tindy Li, Sidney Liang, Qingjie Liu, Donglei Liu, Steven Magnuson, Gretchen Mannelly, David Miller, Eric Mull, Reina Natero, Dennis O’Keefe, Ning Qi, Jill Wood, Nicole Barucci, Marina Breuhaus, Thomas Claus, Michelle Daly, Lynn Lemoine, Yaxin Li, James Livingston, Laurel Sweet, Adrian Tersteegen, Hong Wang, Jian Zhu, Rainer Heurich
Selective PDE11A inhibitors as glucose-dependent insulin secretagogues: Synthesis and SAR of 1,6-naphthyridinones
William Bullock, Libing Chen, Nicole Barucci, Marina Breuhaus, Thomas Claus, Michelle Daly, David Gunn, Lynn Lemoine, Yaxin Li, Qingjie Liu, James Livingston, Laurel Sweet, Adrian Tersteegen, Christopher Town, Hong Wang, Jian Zhu, Rainer Heurich, Yamin Wang
Design, synthesis and relaxant activity of 2-(substituted phenyl)-1H-benzimidazoles on isolated rat aortic rings
Gabriel Navarrete-Vazquez, Samuel Estrada-Soto, Rafael Villalobos-Molina, Ismael Leon-Rivera, Hermenegilda Moreno-Diaz, Mariana Torres-Piedra, Francisco Aguirre-Crespo, Jorge Vergara-Galicia
Structure-activity relationships of 2, N6, 5'-substituted adenosine derivatives as human A2B adenosine receptor agonists
Hayamitsu Adachi, Krishnan K. Palaniappan, Zhan-Guo Gao, Kenneth A. Jacobson
Structure activity relationship of uridine 5′–diphosphoglucose (UDP-glucose) analogs at the human P2Y14 receptor
Hyojin Ko, Ingrid Fricks, Andrei A. Ivanov, T. Kendall Harden, Kenneth A. Jacobson
Structure-activity relationships of carboxylic acid derivatives of PPADS (pyridoxal-5'-phosphate-azo-disulfonic acid) as P2X receptor antagonists
Yong-Chul Kim, Kwan-Young Jung, Ju Yeon Lee, Ga Eun Lee, Hyo Joon Kim
Discovery of tetrahydrofluorenones as a new class of estrogen receptor ß-subtype selective ligands
Robert R Wilkening, Ronald Ratcliffe, Erin Tynebor, Kenneth Wildonger, Amy Fried, Milton Hammond, Ralph Mosley, Paula Fitzgerald, Nandini Sharma, Brian McKeever, Stephan Nilsson, Matts Carlquist, Anne Thorsell, Louis Locco, Robert Katz, Katalin Frisch, Elizabeth Birzin, Hilary Wilkinson, Sudha Mitra, Sheng-Jian Cai, Edward Hayes, James Schaeffer, Susan Rohrer
Tetrahydrofluorenones with conformationally restricted side chains as selective estrogen receptor beta ligands
Kenneth J. Wildonger, Ronald Ratcliffe, Ralph Mosley, Milton L. Hammond, Elizabeth T. Birzin, Susan P. Rohrer
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing A 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators
Puwen Zhang, Jeffrey C. Kern, Eugene A. Terefenko, Andrew Fensome, Ray J Unwalla, Yuan Zhu, Jeff Cohen, Richard C. Winneker, Zhiming Zhang, Jay Wrobel
Establishment of a QSAR model for the prediction of the neuroprotective and antioxidant properties of different estrogen analogs
Nilka M. Rivera, Laszlo Prokai
A useful oral bioavailability/plasma exposure model for 4-(2-phenyl)benzimidazole GnRH antagonists based on a narrow set of physico-chemical molecular properties
Jeffrey C. Pelletier, Daniel Green, Murty V. Chengalvala, Irene B. Feingold, Christine Huselton, Jay Wrobel
Synthesis and biological evaluation of benzoxazole and benzothiazole antagonists of the GnRH receptor
Matthew D. Vera, Murty V. Chengalvala, Joshua E. Cottom, Daniel Green, Diane B. Hauze, Joseph T. Lundquist IV, Charles W. Mann, Jeffrey C. Pelletier, Linda Shanno, Jay Wrobel
Synthesis and evaluation of GnRH receptor antagonists containing piperazinylimidazopyridine and piperazinyltriazolopyridine scaffolds
Joseph T. Lundquist IV, Matthew D. Vera, Jeffrey C. Pelletier, Jay Wrobel, Joshua E. Cottom, Linda Shanno, Murty V. Chengalvala, Christine Huselton, Irene B. Feingold
Structural exploration of a novel class of tricyclic benzodiazepine follicle-stimulating hormone receptor (FSH-R) antagonists: Part I
Amedeo A. Failli, Gavin D. Heffernan, Dominick A. Quagliato, Arthur A. Santilli, Patrick M. Andrae, Richard D. Coghlan, Eugene J. Trybulski, Gi-Chung Chen, Jamin Chi, Tracy L. Owtscharuk, Maria Claudia Perez, Emily S. Shen
Structural exploration of a novel class of tricyclic benzodiazepine follicle-stimulating hormone receptor (FSH-R) antagonists: Part II
Gavin D. Heffernan, Amedeo A. Failli, Dominick A. Quagliato, Arthur A. Santilli, Richard D. Coghlan, Eugene J. Trybulski, Patrick M. Andrae, Gi-Chung Chen, Jamin Chi, Tracy L. Owtscharuk, Maria Claudia Perez, Emily S. Shen
EP4 receptor agonists as ocular hypotensive agents
John Colucci
Biaryl thiazolidin-2,4-diones: A new class of voltage-gated sodium channel blockers for treatment of neuropathic pain
P. K. Chakravarty, C. H. Kuo, S. Tyagarajan, M. Ayer, W. H. Parsons, M. H. Fisher, M. J. Wyvratt, K. A. Lyons, Birgit T. Priest, Richard M. Brochu, I. E. Dick, G. J. Kaczorowski, E. McGowan, Nina Jochnowitz, J. W. Tarpley, S. West, B. S. Reiseter, Catherine Abbadie, W. J. Martin
Synthesis and structure-activity relationships of a series of 5-methyl 5-phenylimidazolidine-2,4-dione derivatives as a Kv1.1/β1 potassium channel disinactivator
Callain Y. Kim, Wayne E. Childers Jr., Boyd L. Harrison, Magid Abou-Gharbia, Mark Bowlby, Flora Jow, Tony Lee, Steve Lin, Mike Monaghan, Kenneth Rhodes, Qiang Wang, Howard Zhang
Paper Withdrawn
Synthesis and SAR study of b-phenylalanine sulfonamide derivatives as bradykinin B1 receptor antagonists for the treatment of pain and inflammation
Nianhe Han, Kaustav Biswas, Lynn Cai, Jennifer Chau, Jian Chen, Derin D'Amico, Christopher H. Fotsch, Aiwen Li, Qingyian Liu, Bobby Riahi, Phi Tang, Chester Yuan, Jiawang Zhu, Gloria Biddlecome, Bob Groneburg, Hsieh Faye, Eileen Johnson, Janan Jona, Smriti Joseph, Gondi Kumar, Dennis Lei, Dianna Lester-Zeiner, Carlo van Staden, Gorden Ng, Ben Askew
Preparation of 2-substituted cyclopropylglycine amide human bradykinin B1 receptor antagonists
Robert M. DiPardo, Ronald K. Chang, Kathy L. Murphy, Richard W. Ransom, Yvonne Leonard, Cuyue Tang, Thomayant Prueksaritanont, Douglas J. Pettibone, Mark G. Bock, Scott D. Kuduk
Potent and orally bioavailable Bradykinin B1 antagonists based on a 5-pyrimidinyl cyclopropanecarboxamide core
Jenny Wai, Neville J. Anthony, Christina Ng Di Marco, Dong-Mei Feng, Robert P. Gomez, Kathy Schirripa, Michael R. Wood, Kathy L. Murphy, Richard W. Ransom, Cuyue Tang, Thomayant Prueksaritanont, Douglas J. Pettibone, Roger M. Freidinger, Mark G. Bock, Scott D. Kuduk
Three dimensional chemical-feature-based pharmacophore development for kappa opioid receptor agonist
Nidhi Singh, Gwénaël Chevé, Christopher R. McCurdy
Paper Withdrawn
Paper Withdrawn
Further modification of aminothiazolomorphinans
Ao Zhang, Zhaohua Yan, John L. Neumeyer, James E. Hilbert, Emily K DeVita, Jean M. Bidlack
Synthesis and preliminary in vitro investigation of carbamate analogs of morphinan pharmacophores at mu, kappa and delta opioid receptors
Xuemei Peng, Brian I. Knapp, Jean M. Bidlack, John L. Neumeyer
Synthesis and preliminary in vitro investigation of bivalent ligands containing hetero-pharmacophores at mu, delta and kappa opioid receptors
Xuemei Peng, Brian I. Knapp, Jean M. Bidlack, John L. Neumeyer
Design, synthesis and evaluation of original 2(3H)-benzoxazolones and 2(3H)-benzothiazolones as highly potent sigma receptor antagonists
Sanju Narayanan, Christophe Mesangeau, Jamal Shaikh, Jie Yu, Jeffery A. Diers, Rae R. Matsumoto, Jacques H. Poupaert, Christopher R. McCurdy
Discovery of an orally available and brain penetrable 6-(piperazine-1-yl)- benzimidazole ORL-1 antagonist
Osamu Okamoto, Kensuke Kobayashi, Hiroshi Kawamoto, Satoru Ito, Atsushi Satoh, Tetsuya Kato, Sayaka Mizutani, Masaya Hashimoto, Atsushi Shimizu, Hiroki Sakoh, Yasushi Nagatomi, Yoshikazu Iwasawa, Hiroyuki Takahashi, Yasuyuki Ishii, Satoshi Ozaki, Hisashi Ohta
Optimization of a benzimidazole series as opioid receptor-like 1 (ORL1) antagonists
Kensuke Kobayashi, Minaho Uchiyama, Hirobumi Takahashi, Hiroshi Kawamoto, Satoru Ito, Takashi Yoshizumi, Hiroshi Nakashima, Tetsuya Kato, Atsushi Shimizu, Hiroshi Miyazoe, Masanori Asai, Akio Ohno, Mioko Hirayama, Satoshi Ozaki, Takeshi Tani, Takeshi Tanaka, Takanobu Mochidome, Kiyoshi Tadano, Fukuroda Takahiro, Osamu Okamoto, Hisashi Ohta
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: Part 1
John Caldwell, Julius Matasi, Hongtao Zhang, April Smith Torhan, Ahmad Fawzi, Deen Tulshian
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: Part 2
John Caldwell, Julius Matasi, Hongtao Zhang, April Smith Torhan, Ahmad Fawzi, Deen Tulshian
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1
Ginny D Ho, Ana Bercovici, Ahmad Fawzi, April Smith Torhan, Deen Tulshian, Hongtao Zhang
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2
Ginny D Ho, Ana Bercovici, Ahmad Fawzi, April Smith Torhan, Deen Tulshian, Hongtao Zhang
Synthesis and structure-activity relationships (SAR) of N-substituted amide spiropiperidines as nociceptin receptor ligands: Part 3
Julius Matasi, John Caldwell, Hongtao Zhang, Ahmad Fawzi, Deen Tulshian, April S. Torhan
Discovery of a cannabinoid-1 receptor PET tracer suitable for clinical use
Ping Liu, Linus S. Lin, Terence G. Hamill, James P. Jewell, Thomas J. Lanza, Stephen M. Krause, Christine Ryan, Waisi Eng, Sandra Sanabria, Raymond E. Gibson, Xinchun Tong, Junying Wang, Tung M. Fong, Julie Lao, Sanjeev Kumar, Wenji Yin, Mark T. Goulet, Richard Hargreaves, H, Donald Burns, William K. Hagmann
Discovery of a novel cannabinoid-1 receptor inverse agonist for the treatment of obesity
William K. Hagmann, Linus S. Lin, Thomas J. Lanza, James P. Jewell, Ping Liu, Shrenik K. Shah, Quang Truong, Hongbo Qi, Ravindra N. Guthikonda, Linda L. Chang, Jonathan Wilson, Helen Armstrong, Ihor E. Kopka, Bing Li, Grace Quaker, Amy Galka, Xinchun Tong, Junying Wang, Sherry Xu, Tung M. Fong, Chun-Pyn Shen, Julie Lao, Jing Chen, Lauren P. Shearman, D. Sloan Stribling, Kimberly Rosko, Alison Strack, Donald J. Marsh, Yue Feng, Sanjeev Kumar, Koppara Samuel, Wenji Yin, Lex H. T. Van der Ploeg, Mark T. Goulet
Synthesis and biological evaluation of novel thiazolo[3,2-a]benzimidazole derivatives as metabotropic glutamate receptor 1 antagonists
Jiro Fujiyasu, Hirotsune Itahana, Masamichi Okada, Takashi Toya, Toshihiro Watanabe, Minoru Okada, Mitsuaki Ohta
Microwave-assisted synthesis of potent mGluR5 antagonists
Bin Shao
Prodrugs of 3-(3,4-dicholorobenzyloxy)-2-amino-6-fluorobicyclo[3.1.0]hexane- 2,6-dicarboxylic acid (MGS0039): Potent and orally active group II mGluR antagonist with antidepressant-like potential
Akito Yasuhara, Masato Nakamura, Kazunari Sakagami, Yasunori Kawakita, Toshiharu Shimazaki, Shigeyuki Chaki, Hiroshi Ohta, Atsuro Nakazato
Design and synthesis of 3,5-bis-benzamide substituted DNK 333 analogs as dual NK-1/NK-2 receptor probes
Vijaya L. Korlipara, Venkat Manoj Swarna, Bradley J. Undem
Series of potent, orally active alpha,alpha-disubstituted piperidine NK1 antagonists
Dong Xiao, Cheng Wang, Gregory Reichard, Hon-Chung Tsui, Sunil Paliwal, Anandan Palani, Neng-Yang Shih, Ruth A. Duffy, Gerard Randolph, Jean Lachowicz, Geoffrey Varty, Cynthia Morgan, Fei Liu, Amin Nomeir
Improving metabolism of novel cyclic urea NK1 antagonists with amine capping groups
Dong Xiao, Carmine Stengone, Gregory Reichard, Neng-Yang Shih, Ruth A. Duffy, Gerard Randolph, Jean Lachowicz, Geoffrey Varty, Cynthia Morgan, Fei Liu, Amin Nomeir
Novel piperidine scaffold as an orally active NK1 antagonist
Jonathan R. Young, Ronsar Eid, Robert J. DeVita, Gary G. Chicchi, Kwei-Lan C Tsao, Marc Kurtz, James V. Pivnichny, Sharon Tong, Song Zheng, Alan Wheeldon, Emma Carlson, Jerry Di Salvo, Ruth Kilburn, Alana Upthagrove, Sanjeev Kumar, Sander G. Mills
Synthesis and biological characterization of the NK2 antagonist SLV332
Daniel P. Jasserand, Holger Sann, Reinhard Brueckner, Dania Reiche, Michael Firnges, Emil Finner, Jochen Antel, Ulf Preuschoff
Novel lipophilic gamma-hydroxybutyrate (GHB) analogs with high affinity to GHB sites in rat brain
Signe Hřg, Petrine Wellendorph, Birgitte Nielsen, Bente Frřlund, Rasmus P. Clausen
Determining the amino acids involved in selective allosteric modulation of the α1β3γ2 and α2β3γ2 GABAAR subtypes
Niki M. Zacharias, Ashutosh A. Kulkarni, Elisha D. Mackey, John B. Nicholas, Mark W. Nowak, Sue Dee Sahba, Nima W. Shiva
Novel hydroxypyrazol-based ligands for characterizing the GABAA binding site
Henriette M. Hansen
Synthesis of isotopically labelled GABA
Robert L. White, Matthew C. Cook
Design and synthesis of novel inhibitors of fatty acid amide hydrolase
Joie Garfunkle, F. Anthony Romero, Dale L. Boger
In vivo imaging of the CRF1 receptors with positron emission tomography
J. S. Dileep Kumar, Gregory M. Sullivan, Ramin V. Parsey, Victoria Arango, Yung-yu Huang, Vattoly J Majo, Jaya Prabhakaran, Ronald L. Van Heertum, J. John Mann
Synthesis of deuterium-labeled antipsychotic drugs
Heiko Junga, Xiangyu Jiang, Christopher James Randlett
Binding selectivity of substituted diarylmethanes to serotonin transporters (SERT)
Balagopal Lakshmi, Seok-Rye Choi, Rajesh Chandra, Zhi-Ping Zhuang, Hank F. Kung
Further structural exploration of tri-substituted asymmetric pyran derivatives, (2S, 4R, 5R)-2-benzhydryl-5-benzylamino-tetrahydropyran-4-ol and their corresponding disubstituted (3S,6S) pyran derivatives: Development of potent molecules for serotonin and norepinephrine transporters
Shijun Zhang, Fernando Fernandez, Stuart Hazeldine, Juan Zhen, Maarten Reith, Aloke Dutta
Synthesis and in vivo evaluation of 5-HT1A receptor agonist radioligand [O-methyl-11C]2-(4-(2-methoxyphenyl)piperazin-1-yl)butyl) -4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates
J. S. Dileep Kumar, Jaya Prabhakaran, Vattoly J Majo, Matthew Milak, Norman R. Simpson, Agata Bukowska, Ronald L. Van Heertum, J. John Mann, Ramin V. Parsey
Synthesis and biological evaluation of a new series of nicotinic acetylcholine receptor (nAChR) ligands for positron emission tomography (PET)
Yongjun Gao, Hayden T Ravert, Daniel Holt, John Hilton, Chris Endres, Mohab Alexander, Anil Kumar, Arman Rahmim, Hiroto Kuwabara, Dean F. Wong, Robert F. Dannals, Andrew G. Horti
Acetylcholine binding proteins (AChBPs) as soluble surrogates of the extracellular ligand binding domain of nicotinic acetylcholine receptors (nAChRs)
Todd T Talley, Palmer Taylor
N-Heteroaryl bridged bicyclic diamines are potent agonists at neuronal nicotinic receptors
William H. Bunnelle, Daniela Barlocco, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Michael J. Dart, Jennifer M. Frost, Arianna Gelain, Jerome F. Daanen, Xenia Searle, David J. Anderson, Pamela Puttfarcken, Jun Chen, Peter Curzon, Michael J. Buckley, Carol S. Surowy
Aryl amide motif with potent D2/5HT2A antagonist activity
James M. Graham, Barr Bridgett, Stephen Cho, Coughenour Linda, Terry Crawford, Tracy F. Gregory, Sham S. Nikam, David Rock, Jamie Singer, Michael A. Walters
Novel sulfonamides having high dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile
G. M. Keserû, É. Ágai-Csongor, J. Galambos, K. Nógrádi, I. Vágó, A. Bielik, B. Kiss, I. Laszlovszky, K. Sághy, J. Laszy, I. Gyertyán, L. Gémesi, M. Zájer-Balázs, Gy. Domány
Positional isomers and bio-isosteric analogs of 7-{[4-(4-Phenyl-piperazin-1-yl)-butyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol for their preferential interaction at the dopamine D3 receptors
Swati Biswas, Juan Zhen, Maarten Reith, Aloke Dutta
Identification of novel, orally-active inhibitors of the TRPV1 (VR1) receptor
Zhi-Liang Wei, Yunfeng Fang, Carl Kaub, Satyanarayana Janagani, Kiran Sahasrabudhe, Guoxhian Wu, John Kincaid, Matthew Duncton, David Lonergan, Nina Orike, Krithika Ramomoorthy, Michelle Dourado, Alejandra Acevedo, Fabien Vincent, David Hackos, Qingling Zhang, Luna Liu, Jennifer Shumilla, Karly Maruyama, Nadia Haque, Tilmann Brotz, Daniel Emerling, Kathleen Martin, Junji Takada, Kazunari Nakao, Katsuhiro Baba, Tetsuhiko Nakagawa, Kenzo Yamamura, Michael Kelly
Design and synthesis of TRPV1 antagonists: Inclusion of a D region binding moiety and a stereocenter
David B. Rusterholz, Karen K. Klyczek, Lucas J. Stolp, Ryan E. Williams, Nicole J. Wellnitz
Tetrahydroquinoline containing ureas as novel transient receptor potential vanilloid 1 (TRPV1) antagonists for the treatment of pain
Robert G. Schmidt, Arthur Gomtsyan, Steven P. Latshaw, Tammie K Jinkerson, Jerome F. Daanen, Heath A. McDonald, Bruce Bianchi, Pamela Puttfarcken, Robert Moreland, Minglei Cui, Prisca Honore, Karen St. George, John F. Darbyshire, Kennan C. Marsh, Teresa Turner, Connie R. Faltynek, Chih-Hung Lee
4-(Pyridin-2-yl)-piperazine-N-hydroxy-1-carboxamidine analogs as TRPV1 antagonists
Xiaoming Zhou, Qun Sun, Donald J. Kyle
Benzoimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists
György Domány, István Borza, Sándor Kolok, Anikó Gere, Kornél Galgóczy, Ildikó Magdó, József Fetter, Ferenc Bertha, Béla Ágai, Csilla Horváth, Sándor Farkas, György M. Keserű
Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands
Robert Aslanian, Xiaohong Zhu, Wing Tom, Wei Zhou, Daniel Solomon, Neng-Yang Shih, John J. Piwinski, Robert West, Shirly M. Williams
Synthesis of optically active subtype selective BZR ligands
Shengming Huang, Clayton Terry, Minghuan Dai, Rahul Edwankar, Chitra Sawant, James M. Cook
3-Normeridamycin: A pNon-immunosuppressive immunophilin ligand is neuroprotective in dopaminergic neurons
Mia Y. Summers, Margaret Leighton, Danni Liu, Kevin Pong, Edmund I. Graziani
Synthesis of fluoro-PEGylated thiophene derivatives for β-amyloid plaque imaging
Rajesh Chandra, Karin Stephenson, Mei-Ping Kung, Catherine Hou, Hank F. Kung
Synthesis of TrkA agonists: Development of therapeutics for treatment of Alzheimer's disease
Rui Zhang, Christine L. Willis, Richard B Sessions, Debbie K Shoemark, Judy J Watson, Mark S Fahey, Gordon K Wilcock, Shelley J Allen, David Dawbarn
Binding sites identification of Abeta-amyloid plaques in Alzheimer's disease based on small molecule ligands
Lisheng Cai, Robert B. Innis, Victor W. Pike
Discovery of cell permeable hydroxyethylamine BACE inhibitors
Roy K. Hom, Michel C. Maillard, Shumeye Mamo, Michael S. Dappen, Louis Brogley, Andrea F. Gailunas, Varghese John, Eugene D. Thorsett, Timothy E. Benson, Danielle D. Woods, D. Bryan Prince, Donna J. Paddock, Thomas L. Emmons, Alfredo G. Tomasselli, Joseph B. Moon
Design and development of cyclic amine BACE1 inhibitors: An overview
Jared Cumming, Lingyan Wang, Suresh Babu, Carolyn Carroll, Xia Chen, Paul Gaspari, William Greenlee, Tao Guo, Doug Hobbs, Ying Huang, Ulrich Iserloh, Matthew Kennedy, Reshma Kuvelkar, Thuy Le, Guoqing Li, Jeffrey Lowrie, Lynne Ozgur, Jianping Pan, Kurt Saionz, Corey Strickland, Andrew Stamford, Dawit Tadesse, Johannes Voigt, Yusheng Wu
Discovery and development of novel BACE-1 inhibitors: Substituted piperidine analogs
Yusheng Wu, Andrew Stamford, Jared Cumming, Ulrich Iserloh, William Greenlee, Matthew Kennedy, Xia Chen, Reshma Kuvelkar, Nansie McHugh, Johannes Voigt, Corey Strickland, Leonard Favreau, Cheng Li, TongTong Liu, Tze-Ming Chan, Rebecca Osterman
Discovery of highly potent piperazine BACE-1 inhibitors
Ying Huang, Xia Chen, William Greenlee, Matthew Kennedy, Reshma Kuvelkar, Guoqing Li, Eric M. Parker, Andrew Stamford, Corey Strickland, Johannes Voigt, Lili Zhang
Discovery of potent pyrrolidine BACE-1 inhibitors
Ulrich Iserloh, Jianping Pan, Alex Buevich, Xia Chen, Jared Cumming, Len Favreau, William Greenlee, Ying Huang, Matthew Kennedy, Reshma Kuvelkar, Nansie McHugh, Guoqing Li, Eric M. Parker, Corey Strickland, Andrew Stamford, Greg Tucker, Johannes Voigt, Lingyan Wang, Yusheng Wu, Ji Zhang, Lili Zhang
Application of diverse computational methods to the optimization of amino-ethanol BACE-1 inhibitors
Johannes Voigt, Jared Cumming, Suresh Babu, Xia Chen, William Greenlee, Tao Guo, Ying Huang, Ulrich Iserloh, Thuy Le, Guoqing Li, Matthew Kennedy, Reshma Kuvelkar, Jianping Pan, Corey Strickland, Dawit Tadesse, Lingyan Wang, Yusheng Wu, Andrew Stamford
Discovery of potent macrocyclic BACE-1 inhibitors
Guoqing Li, Ying Huang, Andrew W. Stamford, William J. Greenlee, Matthew Kennedy, Xia Chen, Reshma Kuvelkar, Corey Strickland, Johannes Voigt
Geometrically constrained p3 amide replacement of beta-secretase inhibitor
Elizabeth F. Stanton, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Ming Chih Crouthamel, Beth L. Pietrak, Ming Tain Lai, Adam J. Simon, Lixia Jin, M. Katherine Holloway, Georgia McGaughey, Samuel L. Graham, Joseph P. Vacca
Solid phase synthesis of competitive BACE inhibitors
Didier JC Berthelot Berthelot, Francois Bischoff, Serge Pieters, Mirielle Braeken, Hans de Winter, Marc Mercken, Ludo Kennis, Lieven Meerpoel
Natural products based beta-secretase inhibitors from Aloe spp. plants and H. occulta
Wei-Shuo Fang, Qing-Yun Yang, Xiao-Yan Tian, Bo Gao, Liang Lv, Chun-Suo Yao, Yue-hua Wang, Guan-hua Du
Systematic comparison of cell permeability between cyclic and linear peptides using reporter gene-based assay
Yong-Uk Kwon, Thomas Kodadek
A peptidomimetic siRNA transfection reagent for highly effective gene silencing in diverse cell types
Yeliz Utku, Ouathek Ouerfelli, Fabio Piano, Ronald N. Zuckermann, Michele Pagano, Kent Kirshenbaum
Synthetic elastic polymer/collagen fibril biocomposite for artificial tissue design
Kerriann Robyn Greenhalgh, Edward Turos, Thomas J. Koob
Use of the 4-hydroxy-1,2,5-oxadiazole-3-yl moiety as novel bioisoster of the distal carboxyl group of the (S)-glutamic acid
Marco L. Lolli, Cecilia Giordano, Birgitte Nielsen, Tommy N. Johansen, Roberta Fruttero, Alberto Gasco
Bisphosphonate binding to farnesyl diphosphate synthase by NMR, X-ray crystallography, calorimetry and quantum chemistry
Fenglin Yin, Sujoy Mukherjee, Junhong Mao, Yong Zhang, Rong Cao, John M. Sanders, Yongcheng Song, Yonghui Zhang, Gary A. Meints, Yi Gui Gao, Dushyant Mukkamala, Michael P. Hudock, Amanda Goddard, Eric Oldfield
Polymeric hollow spheres as controlled drug-delivery vehicles
Zhi-hang Tang, Bao-An Yang
Gold-immobilized cytochrome P450 2C9 metabolism: On chip technology
Peter M. Gannett, Jarod L. Kabulski, Felio A. Perez, Zhongyuan Liu, David Lederman, Charles W. Locuson, Robyn R. Ayscue, Nissa M. Thomsen, Timothy S. Tracy
Synthesis and application of a new molecular probe for the detection of hydroxyl radicals
Amarjit Singh, S. James Adelstein, Amin I. Kassis
Synthesis and guanase inhibition studies of heterocycles and nucleosides containing the imidazo[4,5-d]pyridazine ring system
Ravi K. Ujjinamatada, Ramachandra S. Hosmane
Novel synthesis method of nor-pyrenophorin and other macrodiolides via dilatonization for construction a macrodiolide skeleton
Liu-Lan Shen, Moo-Sung Ko, Jin-Hyun Jeong
Potent antagonists of the Grb2-SH2 domain: Not relying on phosphotyrosine mimics
Sheng Jiang, Peng Li, Megan L. Peach, Robert J. Fisher, Marc C Nicklaus, Peter P. Roller
Rapid synthesis of anhydrous tetrabutylammonium fluoride from potassium fluoride
Haoran Sun, Stephen G. DiMagno
Fluorescent probes to study serine/threonine phosphatases
Fengtian Xue, Christopher T. Seto
Utilizing bound reagents and scavengers with microwave heating, an enabling strategy in medicinal chemistry
Shahnaz Ghassemi
Preparation of novel Pyridine-2-boronic esters, Pyrimidine-4-boronic esters, Pyrazine-2-boronic esters, and Pyridazine-3-boronic esters through palladium-catalyzed cross-coupling reactions
George Y. Li, Xiaomei Qi
Design and synthesis of epoxide peptidomimetics as inhibitors of g-glutamyl hydrolase
Debatosh Majumdar, Matthew D. Alexander, James K. Coward
Visible light-triggered protein inactivation
Jiyong Lee, Peng Yu, Thomas J. Kodadek
Flow cytometry correlation of antigen display and cobalamin uptake in clinically-derived blood samples
Yao Shi, Leah Hartung, David Bahler, Charles B. Grissom
Studies toward synthetically determining a pharmacophore of mitragynine, and indole alkaloid from Mitragyna speciosa: Removal of C-ring
Jessica E. Adkins, Marcelo J. Nieto, Christopher R. McCurdy
Small molecule mass tags for methods of drug discovery
Lori I. Robins, Mark J. Kurth
Medicinal chemistry refinement of a lead compound improves ex vivo metabolic stability with retention of in vivo functions and bioavailability
Laura K. Wing, Hantamalala Ralay Ranaivo, Heather A. Behanna, Wenhui Hu, Sakti M. Roy, Danielle English, D. Martin Watterson
Synthesis and evaluation of ring EB analogs of methyllycaconitine
Bergmeier Stephen C, Junfeng Huang, Dennis B. McKay, Susan McKay
A quantum dot DNA aptamer linked system for detecting proteins
Eric Holwitt, Veronica Franz
Polyketide engineering to supply advanced, complex scaffolds for the construction of high diversity, natural product-like combinatorial libraries
Jasmina Nikodinovic, Bradley A. Bessette Jr., James E Cox, Stephen C. Bergmeier, Mark C. McMills, Nigel D Priestley, Dennis L Wright
Methyl nonactate as a starting scaffold for the parallel synthesis of compound libraries
Stephen C. Bergmeier, Abhijit Nayek, Gregg Wells, Joshua Phillips, P. Whitney Swain III, Bradley A. Bessette Jr., Nigel D. Priestley, Mark C. McMills, Dennis L. Wright
Remote functionalization of the nonactin scaffold via intramolecular insertion
Mark C. McMills, Jason H. Stengel, Stephen C. Bergmeier, Nigel D. Priestley, Dennis L Wright
Fluorescence polarization (FP) assay for identification of vitamin D receptor (VDR) ligands
Steven R. Duff, James G. Farnham, Bryan D. Marks, Naveeda Qadir, Hildegard C. Eliason, Mohammed Saleh Shekhani, Christina Fernandez-Perez, Kurt W. Vogel, William J. Frazee
A new agelasine derivative from the Caribbean sponge Agelas clathrodes
Ivett C. Pina, Phillip Crews, Karen Tenney
Exceptionally facile asymmetric allylboration of aldehydes in water with IPC2Ballyl reagent at high temperatures
Kanth V. B. Josyula, Dinara S. Gunasekera, Sreedhar R. Tummalapalli, Venkata J. Reddy, Pavan K. Mallela, Justin R. Kruger, Venkatram R. Mereddy
Novel synthesis of heterocyclic fluorous b-amino acids using a multifunctional scaffold
Xiaobing Wang Sr., Kit S. Lam
A highly convergent synthesis of the vision pigment A2-E
Murali Mohan Reddy Peram Surakattula, Paul Wentworth Jr.
ALOGPS (http://www.vcclab.org) is a free on-line program to predict lipophilicity and aqueous solubility of chemical compounds
Igor V. Tetko, Vsevolod Y. Tanchuk
Virtual computational chemistry laboratory (VCCLAB) http://www.vcclab.org
Igor V. Tetko, Johann Gasteiger, Roberto Todeschini, Andrea Mauri, David J. Livingstone, Peter Ertl, Vladimir A. Palyulin, Eugene V. Radchenko, Nikolay S. Zefirov, Alexander S. Makarenko, Vsevolod Y. Tanchuk, Volodymyr V. Prokopenko
Effects of omega-3 fatty acids on arachidonate and linoleate product distribution in free radical mediated oxidations
Todd A. Davis, Ned A. Porter
Photophysical and in vitro/in vivo photosensitizing evaluation of 7- and 8-keto bacteriopurpurin-N-alkyl/arylimides derived from Chlorophyll-a
Funda Yukruk, Yihui Chen, Gang Zheng, Andrei N. Kozyrev, Janet Morgan, Ravindra K. Pandey
Synthesis and study of Resolvin D1
Nicos A. Petasis, Jasim Uddin, Charles N. Serhan
Selective (SNAr) arylthiation on aryl substrates bearing multiple substitution sites
Frederick A. Luzzio, Marek T. Wlodarczyk
Effective synthesis for the segment of BILN-2061
Rujian Ma, Wei Miao, Zhiliiu Zhang, Shuhui Chen, Ge Li
Synthetic study toward total synthesis of costunolide
Kun Hu, Han-Seo Mun, Keun-Chul Ryu, Jin-Hyun Jeong
Asymmetric synthesis of cladiellia-6,11-dien-3-ol by IAEA-IMDA strategy: First synthesis of (E)-cladiellin diterpene
Hyoungsu Kim, Hyunjoo Lee, Jayoung Kim, Deukjoon Kim
Solid-phase synthesis of prenylcysteine analogs
James L Donelson, Heather B. Hodges, Christine A. Hrycyna, Richard A. Gibbs
A success story of fragment-based lead generation at Astrazeneca
Loredana Spadola, Morten Hohwy, Karl Edman
Reversed phase C-18 chromatography: From analytical scale to preparative scale
Veronica D. Thomason
Molecular recognition characteristics of riboswitch
Jinsoo Lim, Ronald R. Breaker
Cellular delivery of phosphopeptides by positively-charged tripodal peptides
Guofeng Ye, Nguyen H. Nam, Anil Kumar, Keykavous Parang

Symposium Grid -- Division of Medicinal Chemistry -- Session Listing

Symposium Grid -- Drug Discovery -- Session Listing

The 232nd ACS National Meeting, San Francisco, CA, September 10-14, 2006