Section 43
Chapter 42,483

Cephalosporins. VI. Synthesis and structure-activity relationships of new 7 beta-[ (Z) -2-alkoxyimino-2- (2-aminothiazol-4-yl) acetamido]cephalosporins with a tetraxolopyridazine at the 3-position

Alpegiani, M.; Casabuona, F.; Giorgi, R.; Nannini, G.; Perrone, E.; Meinardi, G.; Bianchi, A.; Monti, G.

Journal of Antibiotics 36(8): 1013-1019


ISSN/ISBN: 0021-8820
PMID: 6630053
Accession: 042482017

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The synthesis and in vitro activity of 7 beta-[(Z)-2-alkoxyimino- 2-(2-aminothiazol-4-yl) acetamido]cephalosporins with a tetrazolo[1,5-b]pyridazine at the 3-position are described. These cephalosporins showed excellent activity against Gram-negative bacteria, including beta-lactamase producing strains. The most interesting compound of the series was 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyimino acetamido] -3-(8-carboxytetrazolo[1,5-b]pyridazin-6-yl)- thiomethyl-3-cephem-4-carboxylic acid (9, FCE 20485) because of its extraordinarily long half-life and marked in vivo activity.

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