Phenylimidazole derivatives as new inhibitors of bacterial enoyl-ACP reductase FabK

Hideo Kitagawa; Tomohiro Ozawa; Sho Takahata; Maiko Iida

doi:10.1016/j.bmcl.2007.06.040

Phenylimidazole derivatives as new inhibitors of bacterial enoyl-ACP reductase FabK

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4982-6. doi: 10.1016/j.bmcl.2007.06.040. Epub 2007 Jun 14.

Authors

Hideo Kitagawa¹, Tomohiro Ozawa, Sho Takahata, Maiko Iida

Affiliation

¹ Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Meiji Seika Kaisha Ltd, Yokohama, Japan. hideo_kitagawa@meiji.co.jp

PMID: 17600706
DOI: 10.1016/j.bmcl.2007.06.040

Abstract

Novel FabK inhibitors with antibacterial activity against Streptococcus pneumoniae were synthesized and evaluated. Through SAR studies of our initial hit compound 2-(1H-benz[d]imidazol-2-ylthio)-N-(6-methoxycarbonylbenzo[d]thiazol-2-yl)acetamide, a series of novel phenylimidazole derivatives were discovered as potent FabK inhibitors.

MeSH terms

Anti-Bacterial Agents / pharmacology
Chemistry, Pharmaceutical / methods*
Drug Design
Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) / antagonists & inhibitors*
Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) / chemistry*
Enzyme Inhibitors / pharmacology*
Imidazoles / chemical synthesis*
Imidazoles / chemistry
Inhibitory Concentration 50
Microbial Sensitivity Tests
Models, Chemical
Streptococcus pneumoniae / enzymology*
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Enzyme Inhibitors
Imidazoles
Enoyl-(Acyl-Carrier-Protein) Reductase (NADH)