CEPHALOSPORINS. II SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF NEW 7-VINYLENETHIOACETAMIDO AND THIOACRYLAMIDO CEPHALOSPORINS

GIULIANO NANNINI; ETTORE PERRONE; DINO SEVERINO; ANGELO BEDESCHI; GIOVANNI BIASOLI; GIUSEPPE MEINARDI; ALBERTA BIANCHI

doi:10.7164/antibiotics.34.412

The Journal of Antibiotics

Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820

CEPHALOSPORINS. II

SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF NEW 7-VINYLENETHIOACETAMIDO AND THIOACRYLAMIDO CEPHALOSPORINS

GIULIANO NANNINI, ETTORE PERRONE, DINO SEVERINO, ANGELO BEDESCHI, GIOVANNI BIASOLI, GIUSEPPE MEINARDI, ALBERTA BIANCHI

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1981 Volume 34 Issue 4 Pages 412-426

DOI https://doi.org/10.7164/antibiotics.34.412

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Abstract

The synthesis and in vitro structure-activity relationships of 7-vinylenethioacetamido and thioacrylamido cephalosporins with various substituents at the 3-position are described. 7(Z)β-Vinylenethioacetamido cephalosporins proved the most active against Gram-positive and Gram-negative bacteria. 7-[(Z)-β-Cyanovinylenethioacetamido]-3-[(1-methyl-1H-tetrazol-5-yl)-thiomethyl]-3-cephem-4-carboxylic acid (K13101, 40) was several times more active in vitro than cefazolin.

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