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1β-甲基-2-[5'-异恶唑并乙烯基吡咯烷-3'-基硫代]碳青霉烯类的合成及生物活性

Synthesis and biological activity of 1beta-methyl-2-[5'-isoxazoloethenylpyrrolidin-3'-ylthio]carbapenems.

作者信息

Kim D J, Seo K J, Lee K S, Shin K J, Yoo K H, Kim D C, Park S W

机构信息

Life Sciences Division, Korea Institute of Science and Technology, Cheongryang, Seoul, South Korea.

出版信息

Bioorg Med Chem Lett. 2000 Dec 18;10(24):2799-802. doi: 10.1016/s0960-894x(00)00575-8.

DOI:10.1016/s0960-894x(00)00575-8
PMID:11133095
Abstract

A new series of 1beta-methylcarbapenems 1a-i bearing isoxazoloethenyl groups on the pyrrolidine ring has been prepared and evaluated for in vitro antibacterial activity and stability to DHP-I. Most compounds showed excellent antibacterial activity and high stability to DHP-I superior to that of meropenem. Of these new carbapenems, 1a,b,h exhibited the best combination of antibacterial activity and DHP-I stability.

摘要

已制备出一系列新的在吡咯烷环上带有异恶唑乙烯基的1β-甲基碳青霉烯类化合物1a-i，并对其体外抗菌活性和对DHP-I的稳定性进行了评估。大多数化合物表现出优异的抗菌活性和对DHP-I的高稳定性，优于美罗培南。在这些新的碳青霉烯类化合物中，1a、b、h在抗菌活性和对DHP-I的稳定性方面表现出最佳组合。

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