SYNTHESIS OF SOME NEW BENZIMIDAZOLECARBOXAMIDES AND EVALUATION OF THEIR ANTIMICROBIAL ACTIVITY

A series of 1,2-disubstituted benzimidazole-5(6)-carboxamides was prep ared and evaluated in vitro for antimicrobial activity against Staphyl occus aureus, Escherichia coli and Candida albicans. The precursor ben zimidazolecarboxylic acids 4a-c and 9a-c were prepared via oxidative c ondensation of diaminobenzoic acids with aldehydes and via several ste ps over the 2(1H)-benzimidazolones, respectively. All acids were conve rted to their acyl chlorides with SOCI2, then amidified with several N ,N'-dialkylaminoethyl derivatives. Compounds 8a-c, 20 and 22 exhibited the best activity. (C) 1998 Elsevier Science S.A. All rights reserved .