STUDIES ON CEPHALOSPORIN ANTIBIOTICS .3. SYNTHESIS, ANTIBACTERIAL ACTIVITY AND ORAL ABSORPTION OF NEW 3-(SUBSTITUTED-ALKYLTHIO)-7-BETA-[(Z)-2-(2-AMINOTHIAZOL-4-YL)-2-(CARBOXYMETHOXYIMINO)ACETAMIDO]CEPHALOSPORINS

被引：5

作者：

YOKOO, C

GOI, M

ONODERA, A

MURATA, M

NAGATE, T

WATANABE, Y

机构：

[1] Research Center, Taisho Pharmaceutical Co., Ltd., Saitama 330, 1-403 Yoshino-cho, Omiya

来源：

JOURNAL OF ANTIBIOTICS | 1991年 / 44卷 / 05期

关键词：

D O I：

10.7164/antibiotics.44.498

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

The synthesis, antibacterial activity and oral absorption in rats of new 7-beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido]cephalosporins (1) having various substituted-alkylthio groups at the C-3 position of the cephem nucleus are described. Of these, the cephalosporins with a cyanomethylthio group (1d) and fluoroethylthio group (1p) at the C-3 position showed a potent in vitro antibacterial activity against Gram-positive and Gram-negative bacteria as well as good oral absorption in rats. When administered orally to mice infected with Klebsiella pneumoniae, 1d had stronger protective effect than 1p. The structure-activity relationships of 1 are also presented.

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页码：498 / 506

页数：9

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