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Discovery of a potent enoyl-acyl carrier protein reductase (FabI) inhibitor suitable for antistaphylococcal agent.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Oct 15; Vol. 25 (20), pp. 4481-6. Date of Electronic Publication: 2015 Sep 03. - Publication Year :
- 2015
-
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.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Dose-Response Relationship, Drug
Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) metabolism
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Methicillin-Resistant Staphylococcus aureus enzymology
Microbial Sensitivity Tests
Molecular Structure
Pyridones chemical synthesis
Pyridones chemistry
Structure-Activity Relationship
Anti-Bacterial Agents pharmacology
Drug Discovery
Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) antagonists & inhibitors
Enzyme Inhibitors pharmacology
Methicillin-Resistant Staphylococcus aureus drug effects
Pyridones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 25
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26343826
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.08.077