6533b838fe1ef96bd12a3d6b
RESEARCH PRODUCT
Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives
Fiorella MeneghettiMaria Valeria RaimondiGiuseppe DaidoneFabiana PlesciaLivia BasileMaria Letizia TrincavelliDemetrio RaffaSalvatore GuccioneBenedetta MaggioClaudia Martinisubject
StereochemistryProtein ConformationChemistry Techniques SyntheticIsochromeno[43-c]pirazoles Dihydrospiro[isoindole-13’-pyrazol]-3(2H)- ones Benzodiazepine receptorDrug DiscoverymedicineAnimalsHumansBenzopyransReceptorBenzodiazepine receptor bindingPharmacologyChemistryOrganic ChemistryGeneral MedicineReceptors GABA-ASettore CHIM/08 - Chimica FarmaceuticaMolecular Docking SimulationMembraneBovine brainActive compoundPyrazolesCattleFlunitrazepam bindingFlunitrazepammedicine.drugProtein Bindingdescription
Abstract 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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2012-01-01 |