Discovery of a potent enoyl-acyl carrier protein reductase (FabI) inhibitor suitable for antistaphylococcal agent

Bioorganic & Medicinal Chemistry Letters
Yun Gyeong KimKye Jung Shin

Abstract

We report the discovery, synthesis, and biological activities of phenoxy-4-pyrone and phenoxy-4-pyridone derivatives as novel inhibitors of enoyl-acyl carrier protein reductase (FabI). Pyridone derivatives showed better activities than pyrone derivatives against FabI and Staphylococcus aureus strains, including methicillin-resistant Staphylococcus aureus (MRSA). Among the pyridone derivatives, compound 16l especially exhibited promising activities against the MRSA strain and good pharmacokinetic profiles.

References

Feb 24, 2001·International Journal of Antimicrobial Agents·R BaxJ Verhoef
Aug 2, 2002·Nature·Helen Pearson
Apr 1, 1995·International Journal of Antimicrobial Agents·A Voss, B N Doebbeling

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Citations

Sep 5, 2020·European Journal of Medicinal Chemistry·Preeti RanaSrinivas Nanduri

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