The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
STUDIES ON CEPHALOSPORIN ANTIBIOTICS
IV. SYNTHESIS, ANTIBACTERIAL ACTIVITY AND ORAL ABSORPTION OF NEW 3-(2-SUBSTITUTED-VINYLTHIO)-7β-[(Z)-2-(2-AMINOTHIAZOL-4-YL)-2-(CARBOXYMETHOXYIMINO)ACETAMIDO]CEPHALOSPORINS
CHIHIRO YOKOOMASAMI GOIAKIRA ONODERAHIROSHI FUKUSHIMATAKATOSHI NAGATE
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1991 Volume 44 Issue 12 Pages 1422-1431

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Abstract

A series of new 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido]cephalosporins (1) having various substituted-vinylthio groups at the C-3 position of the cephem nucleus was synthesized and evaluated for antibacterial activity and oral absorption in rats in comparison with cefixime. Of these, the cephalosporins (1a and 1c) with a lower alkoxycarbonylvinylthio group (Z-form) at the C-3 position showed a potent antibacterial activity against Gram-negative bacteria, improved activity against Staphylococcus aureus as well as good oral absorption in rats. The structure-activity relationships of 1 are also presented.

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