A quantitative structure-activity relationship study on some pyrazolo[4,5-c]quinolines acting as inhibitors of benzodiazepine-receptor binding.
By a quantitative structure-activity relationship (QSAR) study, the ability of a series of 1-arylpyrazolo[4,5-c]quinolin-4-ones to displace specific [3H]-flunitrazepam from bovine brain membranes is shown to be significantly correlated with steric and hydrophobic constants of aryl subtituents, suggesting that substituents of 2- and 6-positions produce dominant steric effects and that those of 3- and 5-positions are involved in strong hydrophobic interaction with the receptor.
Gupta
S P
SP
Birla Institute of Technology and Science, Pilani, India.
Saha
R N
RN
Gupta
J K
JK
Singh
P
P
D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects; D002417:Cattle; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D066298:In Vitro Techniques; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects*; D013329:Structure-Activity Relationship
D011720:Pyrazoles; D015363:Quinolones; D011963:Receptors, GABA-A