Structure-activity relationship studies at the benzodiazepine receptor (BZR): a comparison of the substitutent effects of pyrazoloquinolinone analogs.
The synthesis of a series of 2-phenylpyrazolo[4,3-c]quinolin-3-one derivatives and their in vitro biological evaluation as ligands for the benzodiazepine receptor are described. The in vitro activities, as determined by an analysis of GABA shift ratios, and binding affinities of these compounds to BZR are compared in terms of the electronic, lipophilic, and steric effect changes of their substituents.
Department of Chemistry, Rutgers, State University of New Jersey, Newark 07102.
R I
RI
Fryer
P
P
Zhang
R
R
Rios
Z Q
ZQ
Gu
A S
AS
Basile
P
P
Skolnick
D000818:Animals; D001921:Brain / Q000378:metabolism; D066298:In Vitro Techniques; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000378:metabolism; D015363:Quinolones / Q000138:chemical synthesis* / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D011963:Receptors, GABA-A / Q000378:metabolism*; D012995:Solubility; D013329:Structure-Activity Relationship
D011720:Pyrazoles; D015363:Quinolones; D011963:Receptors, GABA-A