Synthesis and biological evaluation of new indazole derivatives

Abstract

New N-methyl and N-ethyl substitutions in the indazole nucleus are reported by reacting 3-(2-aminobenzamido)indazole and the appropriate trimethyl/triethyl orthobenzoate. Single crystal X-ray analysis confirms the N-ethylation position for the 3-(1-ethyl-1H-indazol-3-yl)-2-phenylquinazolin-4(3H)-one derivative 3f. Compounds 11a-d and 3a-d were tested to evaluate their antimicrobial, antiproliferative and COX inhibitory activities, showing scarce or moderately antiproliferative activity and some inhibitory activity against COX-1 and COX-2. © ARKAT USA, Inc.