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半合成头孢菌素。IV. 肠胃外活性7-[4-(取代甲基)苯基]-乙酰胺基-3-头孢烯-4-羧酸的合成及构效关系

Semisynthetic cephalosporins. IV. Synthesis and structure activity relationships of parenterally active 7-[4-(substituted methyl)phenyl]-acetamido-3-cephem-4-carboxylic acids.

作者信息

Nudelman A, Haviv F, Patchornick A, Karoly-Hafely E, Braun-Bucholts F, Kaier B, Itzchaki J, Sasson S, Erickson R C

出版信息

J Antibiot (Tokyo). 1981 Oct;34(10):1311-7. doi: 10.7164/antibiotics.34.1311.

Abstract

A group of novel 4-substituted phenylacetic acids were prepared and coupled with several 7-amino-delta-3-cephems to afford a family of parenterally active cephalosporins. A compound designated 13I had the broadest spectrum of activity and the highest potency of the group against both Gram-positive and Gram-negative bacteria. The activity of 13I included high potency against penicillinase-producing staphylococci and activity against anaerobes, including Bacteroides fragilis.

摘要

制备了一组新型的4-取代苯乙酸,并将其与几种7-氨基-δ-3-头孢烯偶联,得到了一系列具有肠道外活性的头孢菌素。一种名为13I的化合物具有最广的活性谱,并且在该组中对革兰氏阳性菌和革兰氏阴性菌都具有最高的效力。13I的活性包括对产青霉素酶葡萄球菌的高效力以及对厌氧菌(包括脆弱拟杆菌)的活性。

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