Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives
- Authors: Maggio, B; Raffa, D; Raimondi, MV; Plescia, F; Trincavelli, ML; Martini, C; Meneghetti, F; Basile, L; Guccione, S; Daidone, G
- Publication year: 2012
- Type: Articolo in rivista (Articolo in rivista)
- Key words: Isochromeno[4,3-c]pirazoles, Dihydrospiro[isoindole-1,3’-pyrazol]-3(2H)- ones, Benzodiazepine receptor
- OA Link: http://hdl.handle.net/10447/78361
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.