Phenylimidazole derivatives as new inhibitors of bacterial enoyl-ACP reductase FabK.
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.
Kitagawa
Hideo
H
Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Meiji Seika Kaisha Ltd, Yokohama, Japan. hideo_kitagawa@meiji.co.jp
Ozawa
Tomohiro
T
Takahata
Sho
S
Iida
Maiko
M
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D013296:Streptococcus pneumoniae / Q000201:enzymology*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D007093:Imidazoles; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH)