Section 42
Chapter 41,459

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

Yokoo, C.; Onodera, A.; Fukushima, H.; Numata, K.; Nagate, T.

Journal of Antibiotics 45(6): 932-939


ISSN/ISBN: 0021-8820
PMID: 1500361
DOI: 10.7164/antibiotics.45.932
Accession: 041458690

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A series of new 3-[(Z)-2-methoxycarbonylvinylthio]-7 beta-[(2- aminothiazol-4-yl)acetamido]-cephalosporins (1) having various oxyimino groups (Z-form) at the alpha 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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