RESUMEN
The synthesis and in vitro activity of 7 alpha-methoxy-7 beta-vinylenethioacetamido cephalosporins with various substituents at the 3-position are described. These cephalosporins showed good activity against beta-lactamase producing Gram-negative bacteria. 7 alpha-Methoxy-7-[(Z)-beta-cyano-vinylenethioacetamido]-3-[(1-methyl-1H-tetrazol -5-yl)thiomethyl]-3-cephem-4-carboxylic acid (3) was several times more active in vitro than cefoxitin and comparable to cefmetazole.
Asunto(s)
Cefalosporinas/síntesis química , Bacterias/efectos de los fármacos , Cefalosporinas/farmacología , Fenómenos Químicos , Química , Pruebas de Sensibilidad Microbiana , Relación Estructura-ActividadRESUMEN
The synthesis and in vitro activity of 7-vinylenethioacetamido cephalosporins with a tetrazolo-pyridazine at the 3-position are described. These cephalosporins showed good activity against Gram-positive and Gram-negative bacteria. 7-[(Z)-beta-carboxyvinylenethio-acetamido]-3-[(tetrazolo[1,5-b]pyridazin-8- amino-6-yl)-thiomethyl]-3-cephem-4-carboxylic acid (K 13176, 21) was significantly more active in vitro and in vivo than cefazolin against Gram-negative bacteria.
Asunto(s)
Cefalosporinas/síntesis química , Cefalosporinas/farmacología , Fenómenos Químicos , Química , Pruebas de Sensibilidad Microbiana , Relación Estructura-ActividadRESUMEN
A series of 7-substituted alkyl-thio-acylaminocephalosporins with the following general formula were prepared and tested for in vitro antibacterial activity: (formula: see text). We tried in our research to find any relationship between antibacterial activity and pharmacokinetic properties on the one hand, and chemical structure on the other. The most interesting products were also studied for their in vivo antibacterial activity in experimental acute systemic infections in the mouse.