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.
Synthesis and biological evaluation of new indazole derivatives / S. Plescia, D. Raffa, F. Plescia, G. Casula, B. Maggio, G. Daidone, M.V. Raimondi, M.G. Cusimano, G. Bombieri, F. Meneghetti. - In: ARKIVOC. - ISSN 1551-7004. - 2010:part 10(2010), pp. 156-164.
Synthesis and biological evaluation of new indazole derivatives
G. BombieriPenultimo
;F. MeneghettiUltimo
2010
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.
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