Quantitative structure-activity relationship study on some ligands acting as inhibitors of benzodiazepine-receptor binding.

Previously reported quantitative structure-activity study on 1-aryl-3-methylpyrazolo[4,5-c]quinolin-4-ones is extended to include recently reported 1-aryl[1]benzopyrano-pyrazol-4-ones. It has been shown that the ability of these compounds to displace [3H]-flunitrazepam from bovine brain membrane is significantly correlated with steric and hydrophobic constants of aryl substituents. For 1,3-diaryl-pyrazolo[4,5-c]quinolin-4-ones, however, only hydrophobic interaction of meta-substituents is found to be relevant.