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7β-[(Z)-2-(2-氨基噻唑-4-基)-3-(取代基)-2-丙烯酰氨基]-3-去乙酰氧甲基头孢菌素的合成及构效关系

Synthesis and structure-activity relationships of 7 beta-[(Z)-2-(2- aminothiazol-4-yl)-3-(substituted)-2-propenoyl-amino]-3- desacetoxymethylcephalosporins.

作者信息

Ishikura K, Kubota T, Minami K, Hamashima Y, Nakashimizu H, Motokawa K, Yoshida T

机构信息

Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan.

出版信息

J Antibiot (Tokyo). 1994 Apr;47(4):453-65. doi: 10.7164/antibiotics.47.453.

Abstract

Synthesis and biological activity of a series of 7 beta-[(Z)-2-(2- aminothiazol-4-yl)-3-(substituted)-2-propenoylamino]-3-cephe m-4-carboxylic acids and their pivaloyloxymethyl esters are described. These acid compounds exhibited potent antibacterial activity against both Gram-positive and Gram-negative bacteria. Pivaloyloxymethyl esters of selected compounds in this series were found to be well absorbed from small intestine in mice.

摘要

描述了一系列7β-[(Z)-2-(2-氨基噻唑-4-基)-3-(取代基)-2-丙烯酰氨基]-3-头孢烯-4-羧酸及其新戊酰氧甲基酯的合成和生物活性。这些酸化合物对革兰氏阳性菌和革兰氏阴性菌均表现出强效抗菌活性。发现该系列中所选化合物的新戊酰氧甲基酯在小鼠小肠中吸收良好。

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