MEDI 13 |
| We seek to design, synthesize, and evaluate peptidomimetic ligands as new probes to modulate bacterial quorum sensing (QS). There is an urgent, global need for new antimicrobial therapies, and the regulation of QS has emerged as a highly attractive target. QS is a process of bacterial intercellular communication. Using signaling molecules and their cognate receptors, bacteria monitor their population density and regulate group behaviors, such as virulence and biofilm formation. We hypothesize that peptidomimetics of these ligands could represent valuable tools to modulate QS and attenuate pathogenesis. In Gram-positive bacteria, these ligands are short peptides; thus we designed N-substituted glycine oligomer, or peptoid, mimics. We have prepared focused libraries of linear and macrocyclic peptoids and peptide-peptoid hybrids (peptomers) in high yield and purity utilizing microwave-assisted reaction conditions. This talk will present our on-going characterization of these ligands in QS assays in Staphylococcus aureus. |
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Medicinal Chemistry Award Symposium
1:30 PM-4:20 PM, Sunday, August 19, 2007 BCEC -- 210B, Oral
Division of Medicinal Chemistry |