Structure-activity relationship studies at benzodiazepine receptor (BZR): a comparison of the substituent effects of pyrazoloquinolinone analogs

…, R Rios, ZQ Gu, AS Basile, P Skolnick

Index: Fryer; Zhang; Rios; Gu; Basile; Skolnick Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1669 - 1673

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Citation Number: 57

Abstract

The synthesis of a series of 2-phenylpyrazolo [4, 3-clquinolin-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 BZRare compared in terms of the electronic, lipophilic, and steric effect changes of their substituents.