C-2位季碳杂环烷硫基碳青霉烯类化合物的合成及其体外活性

Synthesis and in vitro activity of C-2 quaternary heterocyclic alkylthio carbapenems.

作者信息

Kim C U, Misco P F, Luh B Y, Hitchcock M J

机构信息

Bristol-Myers Company, Pharmaceutical Research and Development Division, Wallingford, CT 06492-7660.

出版信息

J Antibiot (Tokyo). 1987 Dec;40(12):1707-15. doi: 10.7164/antibiotics.40.1707.

DOI:10.7164/antibiotics.40.1707

PMID:3429337

Abstract

The synthesis of new carbapenems having various (substituted) quaternary heterocyclic alkylthio groups at the C-2 position is described. The in vitro antibacterial activity and the dehydropeptidase-I susceptibility were examined. Some of these compounds (e.g., 11, 16, 26 and 27) showed an excellent wide spectrum of in vitro antibacterial activity including activity against Pseudomonas aeruginosa and greater stability than imipenem toward the dehydropeptidase-I.

摘要

描述了在C-2位具有各种（取代的）季铵杂环烷硫基的新型碳青霉烯类化合物的合成。检测了其体外抗菌活性和对脱氢肽酶-I的敏感性。其中一些化合物（如11、16、26和27）表现出优异的广谱体外抗菌活性，包括对铜绿假单胞菌的活性，并且比亚胺培南对脱氢肽酶-I具有更高的稳定性。