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β-内酰胺抗生素的研究。IV. 3-(异噻唑基硫甲基)头孢菌素的改进合成及其在新衍生物中的应用。

Studies on beta-lactam antibiotics. IV. An improved synthesis of 3-(isothiazolylthiomethyl)cephalosporins and its application to new derivatives.

作者信息

Hara R, Nakai E, Hisamichi H, Nagano N

机构信息

Infectious Disease and Immunology Research Laboratories, Yamanouchi Pharmaceutical Co., LTD., Ibaraki, Japan.

出版信息

J Antibiot (Tokyo). 1994 Apr;47(4):477-86. doi: 10.7164/antibiotics.47.477.

DOI:10.7164/antibiotics.47.477
PMID:8195048
Abstract

An improved synthesis and in vitro activity of cephalosporins with a (4-carboxy-3-hydroxy-5-isothiazolyl)thiomethyl group at the 3-position and its application to the preparation of new derivatives are described. These compounds showed excellent activity against Gram-negative bacteria including beta-lactamase producing strains. Among them, 2f was the most interesting because of its broad spectrum of antibacterial activity, including Gram-positive bacteria, and its outstanding inhibitory potency against Pseudomonas aeruginosa.

摘要

描述了3位带有(4-羧基-3-羟基-5-异噻唑基)硫甲基的头孢菌素的改进合成方法、体外活性及其在制备新衍生物中的应用。这些化合物对包括产β-内酰胺酶菌株在内的革兰氏阴性菌显示出优异的活性。其中,2f最为引人关注,因为它具有广谱抗菌活性,包括对革兰氏阳性菌,并且对铜绿假单胞菌具有出色的抑制效力。

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