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Studies on cephalosporin antibiotics. II. Synthesis, antibacterial activity and oral absorption of 3-alkoxycarbonylmethoxy-7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)-acetamido]cephalosporins.

作者信息

Yokoo C, Goi M, Onodera A, Murata M, Nagate T, Watanabe Y, Sota K

机构信息

Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.

出版信息

J Antibiot (Tokyo). 1988 Feb;41(2):181-92. doi: 10.7164/antibiotics.41.181.

DOI:10.7164/antibiotics.41.181
PMID:3356606
Abstract

The synthesis, antibacterial activity and oral absorption in rats of 3-alkoxycarbonyl-methoxy-7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)acetamido]cephalosporins (1) are described. In this cephalosporin series, 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(carboxy-methoxyimino)acetamid o] cephalosporins (1b, 1i and 1j) with a lower alkoxycarbonylmethoxy group at the C-3 position of a cephem nucleus exhibited not only potent activity against Gram-negative bacteria but also good oral absorption in rats. Structure-activity relationships of 1 are also presented.

摘要

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