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|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
|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.
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