6533b820fe1ef96bd1279cb7

RESEARCH PRODUCT

Synthesis and biological evaluation of new indazole derivatives

Giovanni CasulaFiorella MeneghettiGiuseppe DaidoneMaria Grazia CusimanoGabriella BombieriFabiana PlesciaDemetrio RaffaSalvatore PlesciaBenedetta MaggioMaria Valeria Raimondi

subject

IndazoleStereochemistryOrganic Chemistrybiological activityBiological activityAntimicrobialSettore CHIM/08 - Chimica Farmaceuticalcsh:QD241-441chemistry.chemical_compoundN-methyl/N-ethyl alkylationlcsh:Organic chemistry4(3H)-quinazolinonechemistryindazolecrystallographyBiological evaluation

description

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.

yearjournalcountryeditionlanguage
2010-07-29Arkivoc
https://doi.org/10.3998/ark.5550190.0011.a14