A series of isochromeno[4,3-c]pyrazole-5(1H)-one derivatives 7b-h were prepared and tested at 10 μM 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 7a-d,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14a-d,i, showing that the isochromene/chromene isomerism influences the activity.
|Titolo:||Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives|
|Parole Chiave:||Isochromeno[4,3-c]pirazoles; Dihydrospiro[isoindole-1,3 '-pyrazol]-3(2H)-ones; Benzodiazepine receptor|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
|Data di pubblicazione:||2012|
|Digital Object Identifier (DOI):||10.1016/j.ejmech.2012.06.028|
|Appare nelle tipologie:||01 - Articolo su periodico|