Antimicrobial substd.-3-cephem-4-carboxylic acid - with better activity, tissue distribution, bile secretion and protecting activity than known cephalexine

摘要

7-(3-Alkanesulphonamidophenyl-D-glycinamido)-3-methyl-3-cephem-4-- carboxylic acid of formula (I) or its salts, is prepd. by reacting 7-amino-3-methyl-3-cephem-4-carboxylic acid (II) or its salt with 3-alkanesulphonamidophenyl-glycine (III) or its carboxy deriv. in the presence of a liquid culture or its worked-up material of a micro-organism which is able to N-acylate (II) with (III). (where R = alkyl (1-6C, pref. 1-4C) (I) is an antimicrobial agent for oral use with a high activity against pathogenous micro-organisms esp. Klebsiella pneumonia and Proteus mirabilis. The activity, blood levels, tissue distribution bile-secretion and protecting activity on experimental infected mice of (I) are better than those of known cephalexine.