High affinity central benzodiazepine receptor ligands. Part 3: Insights into the pharmacophore and pattern recognition study of intrinsic activities of pyrazolo [4, 3-c] …

A Carotti, C Altomare, L Savini, L Chiasserini…

Index: Carotti, Andrea; Altomare, Cosimo; Savini, Luisa; Chiasserini, Luisa; Pellerano, Cesare; Mascia, Maria P.; Maciocco, Elisabetta; Busonero, Fabio; Mameli, Manuel; Biggio, Giovanni; Sanna, Enrico Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 23 p. 5259 - 5272

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Citation Number: 25

Abstract

Novel 2-phenyl-2, 5-dihydropyrazolo [4, 3-c] quinolin-3-(3H)-ones (PQs) endowed with high affinity for central benzodiazepine receptor (BzR) were synthesized. In particular, 9-fluoro-2- (2-fluorophenyl)-2, 5-dihydro-3H-pyrazolo [4, 3-c] quinolin-3-one (22) showed binding affinity in the subnanomolar concentration range and proved to be in vitro a potent antagonist. This finding allowed the nature of the hydrogen bonding receptor site H2 to be ...