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GIUSEPPE DAIDONE

Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives

  • Autori: Maggio, B.; Raffa, D.; Raimondi, M.; Plescia, F.; Trincavelli, M.; Martini, C.; Meneghetti, F.; Basile, L.; Guccione, S.; Daidone, G.
  • Anno di pubblicazione: 2012
  • Tipologia: Articolo in rivista (Articolo in rivista)
  • Parole Chiave: Isochromeno[4,3-c]pirazoles, Dihydrospiro[isoindole-1,3’-pyrazol]-3(2H)- ones, Benzodiazepine receptor

Abstract

for their ability to displace specific [3H]flunitrazepam from bovine brain membranes. The substitution pattern of the above derivatives was shown to influence the receptor affinity. The most active compound of the series was 7e, showing a 54% inhibition of [3H]flunitrazepam binding. Compounds 7aed,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14aed,i, showing that the isochromene/chromene isomerism influences the activity.

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