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莫西拉坦(6059-S),一种新型1-氧杂-β-内酰胺:对大肠杆菌K-12青霉素结合蛋白的结合亲和力。

Moxalactam (6059-S), a new 1-oxa-beta-lactam: binding affinity for penicillin-binding proteins of Escherichia coli K-12.

作者信息

Komatsu Y, Nishikawa T

出版信息

Antimicrob Agents Chemother. 1980 Mar;17(3):316-21. doi: 10.1128/AAC.17.3.316.

Abstract

Moxalactam (6059-S) is a new beta-lactam derivative with a structure markedly different from those of penicillins or cephalosporins. The binding activity of 6059-S to penicillin-binding proteins (PBPs) in Escherichia coli K-12 was tested. [14C]benzylpenicillin- or [14C]6059-S-bound inner membrane proteins of E. coli K-12 were rapidly detected without using fluorography. 6059-S had the highest affinity for PBP-3 and -7/8, had a higher affinity than benzylpenicillin for PBP-1A, -1Bs, -4, and -5/6 and a lower affinity for PBP-2, 609134, the 1-thiacephem analog of 6059-S, showed as high an affinity for PBP-1A, -1Bs, -3, and -4 as 6059-S but a lower affinity for PBP-5/6.

摘要

莫西拉酸(6059-S)是一种新型β-内酰胺衍生物,其结构与青霉素或头孢菌素显著不同。测试了6059-S对大肠杆菌K-12中青霉素结合蛋白(PBPs)的结合活性。无需使用荧光自显影技术即可快速检测到[14C]苄青霉素或[14C]6059-S结合的大肠杆菌K-12内膜蛋白。6059-S对PBP-3和-7/8具有最高亲和力,对PBP-1A、-1Bs、-4和-5/6的亲和力高于苄青霉素,对PBP-2的亲和力较低,609134是6059-S的1-硫杂头孢菌素类似物,对PBP-1A、-1Bs、-3和-4的亲和力与6059-S一样高,但对PBP-5/6的亲和力较低。

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