Bioorganic and Medicinal Chemistry p. 389 - 399 (1998)
Update date:2022-07-30
Topics:
Savini
Massarelli
Nencini
Pellerano
Biggio
Maciocco
Tuligi
Carrieri
Cinone
Carotti
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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