Sugawara Akihiro, Sunazuka Toshiaki, Hirose Tomoyasu, Nagai Kenichiro, Yamaguchi Yukie, Hanaki Hideaki, Sharpless K Barry, Omura Satoshi
Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, Japan.
Bioorg Med Chem Lett. 2007 Nov 15;17(22):6340-4. doi: 10.1016/j.bmcl.2007.08.068. Epub 2007 Sep 1.
An erythromycin analogue, 11,12-di-O-iso-butyryl-8,9-anhydroerythromycin A 6,9-hemiketal (1b), was found to be a potential anti-MRSA and anti-VRE agent. The use of copper catalyzed azide-acetylene cycloaddition, and click chemistry, readily provided 10 types of triazole analogues of 1b in good to nearly quantitative yield. Among the library, 5b exhibited activity against MRSA and VRE bacterial strains, representing more than twice the potency of 1b.
一种红霉素类似物，11,12-二-O-异丁酰基-8,9-脱水红霉素A 6,9-半缩酮（1b），被发现是一种潜在的抗耐甲氧西林金黄色葡萄球菌（MRSA）和抗耐万古霉素肠球菌（VRE）药物。使用铜催化的叠氮化物-乙炔环加成反应（点击化学），能够轻松地以良好至几乎定量的产率提供10种1b的三唑类似物。在该文库中，5b对MRSA和VRE细菌菌株表现出活性，其效力是1b的两倍多。
