Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3565-9. doi: 10.1016/j.bmcl.2008.05.004. Epub 2008 May 4.

Abstract

Enoyl-ACP reductase (ENR), the product of the FabI gene, from Bacillus anthracis (BaENR) is responsible for catalyzing the final step of bacterial fatty acid biosynthesis. A number of novel 2-pyridone derivatives were synthesized and shown to be potent inhibitors of BaENR.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Bacillus anthracis / drug effects
  • Bacillus anthracis / enzymology*
  • Crystallography, X-Ray
  • Drug Design
  • Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) / antagonists & inhibitors*
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Structure
  • Molecular Weight
  • Pyridones / chemical synthesis*
  • Pyridones / chemistry
  • Pyridones / pharmacology
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Pyridones
  • 2-hydroxypyridine
  • Enoyl-(Acyl-Carrier-Protein) Reductase (NADH)