Ozawa Tomohiro, Kitagawa Hideo, Yamamoto Yasuo, Takahata Sho, Iida Maiko, Osaki Yumi, Yamada Keiko
Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd, 760 Morooka-cho, Kohoku-ku, Yokohama 222-8567, Japan.
Bioorg Med Chem. 2007 Dec 1;15(23):7325-36. doi: 10.1016/j.bmc.2007.08.050. Epub 2007 Sep 4.
Bacterial enoyl-acyl carrier protein (ACP) reductases (FabI and FabK) catalyze the final step in each cycle of bacterial fatty acid biosynthesis and are attractive targets for the development of new antibacterial agents. Here, we report the development of novel FabK inhibitors with antibacterial activity against Streptococcus pneumoniae. Based on structure-activity relationship (SAR) studies of our screening hits, we have developed novel phenylimidazole derivatives as potent FabK inhibitors.
细菌烯酰-酰基载体蛋白（ACP）还原酶（FabI和FabK）催化细菌脂肪酸生物合成每个循环的最后一步，是开发新型抗菌剂的有吸引力的靶点。在此，我们报告了对肺炎链球菌具有抗菌活性的新型FabK抑制剂的开发情况。基于对筛选命中物的构效关系（SAR）研究，我们开发了新型苯基咪唑衍生物作为有效的FabK抑制剂。
