The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
STUDIES ON CEPHALOSPORIN ANTIBIOTICS
V. SYNTHESIS, ANTIBACTERIAL ACTIVITY AND ORAL ABSORPTION OF NEW 3-[(Z)-2-METHOXYCARBONYLVINYLTHIO]-7β-[(Z)-2-(2-AMINOTHIAZOL-4-YL)-2-(OXYIMINO)ACETAMIDO]CEPHALOSPORINS
CHIHIRO YOKOOAKIRA ONODERAHIROSHI FUKUSHIMAKAZUO NUMATATAKATOSHI NAGATE
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1992 年 45 巻 6 号 p. 932-939

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A series of new 3-[(Z)-2-methoxycarbonylvinylthio]-7β-[(2-aminothiazol-4-yl)acetamido]cephalosporins (1) having various oxyimino groups (Z-form) at the α position of the C-7 side chain was synthesized and evaluated for antibacterial activity and oral absorption in rats. Of these, the cephalosporin (1a) with a hydroxyimino group in the C-7 side chain showed a potent antibacterial activity against Gram-negative bacteria and Gram-positive Staphylococcus aureus as well as good oral absorption in rats. The structure-activity relationships of 1 are also presented.
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© Japan Antibiotics Research Association
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