Oh Chang-Hyun, Dong Hyun-Gu, Lee Joo-Shin, Lee Su-Chul, Hong Joon Hee, Cho Jung-Hyuck
Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul 130-650, Korea.
Arch Pharm (Weinheim). 2003 Dec;336(12):567-72. doi: 10.1002/ardp.200300768.
Synthesis of a new series of 1beta-methylcarbapenems with a substituted oxadiazolopyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of the substituent on the oxadiazole ring investigated. In particular, compounds 13a and 13c with ester and carbamoyl substituted oxadiazole moieties showed the most potent antibacterial activity.
描述了一系列带有取代恶二唑并吡咯烷部分的新型1β-甲基碳青霉烯类化合物的合成。测试了它们对革兰氏阳性菌和革兰氏阴性菌的体外抗菌活性,并研究了恶二唑环上取代基的影响。特别地,带有酯基和氨基甲酰基取代恶二唑部分的化合物13a和13c表现出最强的抗菌活性。