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Synthesis and biological evaluation of new indazole derivatives

  • Autori: Plescia, S.; Raffa, D.; Plescia, F.; Casula, G.; Maggio, B.; Daidone, G.; Raimondi, M.; Cusimano, M.; Bombieri, G.; Meneghetti, F.
  • Anno di pubblicazione: 2010
  • Tipologia: Articolo in rivista (Articolo in rivista)
  • Parole Chiave: N-methyl/N-ethyl alkylation; 4(3H)-quinazolinone; indazole; crystallography; biological activity


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.