4-Pyridone derivatives as new inhibitors of bacterial enoyl-ACP reductase FabI.
Bacterial FAS provides essential fatty acids for use in the assembly of key cellular components. Among them, FabI is an enoyl-ACP reductase which catalyzes the final and rate-limiting step of bacterial FAS. It is a potential target for selective antibacterial action, because it shows low overall sequence homology with mammalian enzymes. Until today, various compounds have been reported as inhibitors of bacterial FabI-inhibitory compounds. To discover novel small-molecular FabI inhibitors, we initially screened our compound library for inhibitory activity toward FabI of Escherichia coli. And discovered 4-pyridone derivatives as a lead compound. Structure optimization studies yielded 4-pyridone derivatives 7n having strong FabI-inhibitory and antibacterial activities against Staphylococcus aureus. There have been no reports concerning 4-pyridone derivatives as FabI inhibitor.[1]References
- 4-Pyridone derivatives as new inhibitors of bacterial enoyl-ACP reductase FabI. Kitagawa, H., Kumura, K., Takahata, S., Iida, M., Atsumi, K. Bioorg. Med. Chem. (2007) [Pubmed]
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