Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/4287
Title: High affinity central benzodiazepine receptor ligands: synthesis and structure-activity relationship studies of a new series of pyrazolo[4,3-c]quinolin-3-ones
Authors: Savini, Luisa
Massarelli, Paola
Nencini, Cristina
Pellerano, Cesare
Biggio, G.
Maciocco, A.
Tuligi, G.
Carrieri, A.
Cinone, N.
Carotti, A.
Keywords: Central benzodiazepine receptor ligands; pyrazolo[4; 3-c]quinolin-3-ones; QSAR; 35S-TBPS binding; pharmacophore refinement
Issue Date: 1998
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY
Abstract: 
A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones, carrying appropriate substituents at the quinoline and N2-phenyl rings, were prepared and tested as central benzodiazepine receptor ligands. Results from structure┬▒affinity relationship studies were in full agreement with previously proposed pharmacophore models and, in addition, quantitative structure-activity analysis gave further significant insight into the main molecular determinants of high benzodiazepine receptor affinity. The intrinsic activity of some active ligands was also determined and preliminary discussed.
Description: 
20791
URI: http://hdl.handle.net/20.500.12779/4287
ISSN: 0968-0896
DOI: 10.1016/S0968-0896(97)10039-6
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