Synthesis and structure-activity relationships of new 7 beta -(Z)-2-alkoxyimino-2-(2-aminothiazol-4-yl)acetamido)-cephalosporin s with a tetrazolopyridazine at the 3-position

The synthesis and in vitro activity of 7 beta -(Z)-2-alkoxyimino-2-(2-aminothiazol-4-yl)acetamido) cephalosporins with a tetrazole(1,5-b)pyridazine at the 3-position are described. These cephalosporins showed excellent activity agaist Gram-negative bacteria, including beta -lactamase producing strai...

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Published inJournal of antibiotics Vol. 36; no. 8; pp. 1013 - 1019
Main Authors Alpegiani, M, Casabuona, F, Giorgi, R, Nannini, G, Perrone, E, Meinardi, G, Bianchi, A, Monti, G
Format Journal Article
LanguageEnglish
Published 01.01.1983
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Summary:The synthesis and in vitro activity of 7 beta -(Z)-2-alkoxyimino-2-(2-aminothiazol-4-yl)acetamido) cephalosporins with a tetrazole(1,5-b)pyridazine at the 3-position are described. These cephalosporins showed excellent activity agaist 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-methoxylimino 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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ISSN:0021-8820