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

作者：Kim Yun Gyeong; Seo Jae Hong; Kwak Jin Hwan; Shin Kye Jung^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(20): 4481-4486.

DOI：10.1016/j.bmcl.2015.08.077

• Enoyl-acyl carrier protein reductase (FabI)
• Antibiotic
• MRSA
• Pyridone

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.

• 出版日期2015-10-15