MEDI 325 |
| There is a pressing need for new antibacterial agents that act via new targets. Bacterial fatty acid biosynthesis enzymes offer such an opportunity. In certain pathogenic bacteria the enoyl-acyl carrier protein (ACP) reductase FabI is responsible for the terminal step in fatty acid biosynthesis and its corresponding gene is essential (similar transformations in humans are carried out by a single multifunctional enzyme designated FAS1). This has led to the pursuit of specific enoyl-ACP reductase inhibitors of FabI as novel antibacterial agents. Structure guided design and synthesis of a series of ene-amide inhibitors of FabI will be described. High resolution 3-dimensional structures of FabI from S. aureus and the Class A pathogen F. Tularensis provide a detailed understanding of the structural factors governing ligand recognition. The potent antibacterial activity of these compounds will be presented. |
|
Fatty Acid Synthase Inhibitors as Anticancer, Antibacterial and Antiparasitic Agents
9:00 AM-11:30 AM, Thursday, April 10, 2008 Morial Convention Center -- La Nouvelle, Blrm. A/B, Oral
Division of Medicinal Chemistry |