doi: 10.1016/j.bmcl.2015.08.077.
Epub 2015 Sep 3.
Discovery of a potent enoyl-acyl carrier protein reductase (FabI) inhibitor suitable for antistaphylococcal agent
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- PMID: 26343826
- DOI: 10.1016/j.bmcl.2015.08.077
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Discovery of a potent enoyl-acyl carrier protein reductase (FabI) inhibitor suitable for antistaphylococcal agent
Bioorg Med Chem Lett.
.
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.
Keywords: Antibiotic; Enoyl-acyl carrier protein reductase (FabI); MRSA; Pyridone.
Copyright © 2015 Elsevier Ltd. All rights reserved.
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