High affinity central benzodiazepine receptor ligands. Part 2: quantitative structure–activity relationships and comparative molecular field analysis of pyrazolo [4, 3-c] …

L Savini, L Chiasserini, C Pellerano, G Biggio…

Index: Savini; Chiasserini; Pellerano; Biggio; Maciocco; Serra; Cinone; Carrieri; Altomare; Carotti Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 2 p. 431 - 444

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Citation Number: 18

Abstract

A large series of 2-aryl (heteroaryl)-2, 5-dihydropyrazolo [4, 3-c] quinolin-3 (3H)-ones (PQ, 106 compounds), carrying appropriate substituents at the quinoline and N2-phenyl rings, were designed, prepared and tested as central benzodiazepine receptor ligands. Compounds with an affinity significantly higher than the parent compound CGS-8216 were obtained, the most active ligand showing a pIC50= 10.35. Hansch and comparative ...