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, their antiproliferative activity and their COX inhibitory activities showing scarce or moderately antiproliferative activity and some inhibitory activity against COX-1 and COX-2.
Plescia, S., Raffa, D., Plescia, F., Casula, G., Maggio, B., Daidone, G., et al. (2010). Synthesis and biological evaluation of new indazole derivatives. ARKIVOC, 2010(X), 163-177 [10.3998/ark.5550190.0011.a14].
Synthesis and biological evaluation of new indazole derivatives
PLESCIA, Salvatore;RAFFA, Demetrio;PLESCIA, Fabiana;CASULA, Giovanni;MAGGIO, Benedetta;DAIDONE, Giuseppe;RAIMONDI, Maria Valeria;CUSIMANO, Maria Grazia;
2010-01-01
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, their antiproliferative activity and their COX inhibitory activities showing scarce or moderately antiproliferative activity and some inhibitory activity against COX-1 and COX-2.
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