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.
Singh
P
P
Department of Chemistry, S.K. Government College, Sikar, India.
Ojha
T N
TN
Sharma
R C
RC
D000818:Animals; D001667:Binding, Competitive; D002417:Cattle; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005445:Flunitrazepam / Q000378:metabolism; D066298:In Vitro Techniques; D008024:Ligands; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism*; D012044:Regression Analysis; D013329:Structure-Activity Relationship
D008024:Ligands; D011963:Receptors, GABA-A; D005445:Flunitrazepam