HIGH-AFFINITY CENTRAL BENZODIAZEPINE RECEPTOR LIGANDS - SYNTHESIS ANDSTRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF A NEW SERIES OF PYRAZOLO[4,3-C]QUINOLIN-3-ONES

A large series of l)-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones, c arrying appropriate substituents at the quinoline and N-2-phenyl rings , were prepared and tested as central benzodiazepine receptor ligands. Results from structure-affinity relationship studies were in full agr eement with previously proposed pharmacophore models and, in addition, quantitative structure-activity analysis gave further significant ins ight into the main molecular determinants of high benzodiazepine recep tor affinity. The intrinsic activity of some active ligands was also d etermined and preliminary discussed. (C) 1998 Published by Elsevier Sc ience Ltd. All rights reserved.