0000000000867035
AUTHOR
Maria Letizia Trincavelli
Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives
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.
ChemInform Abstract: Synthesis, Benzodiazepine Receptor Binding and Molecular Modelling of Isochromeno[4,3-c]pyrazol-5(1H)-one Derivatives.
A series of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives (III) is prepared and tested for their ability to displace specific [3H]flunitrazepam from bovine brain membranes.