77779-98-7Relevant academic research and scientific papers
THERAPEUTIC PYRAZOLOQUINOLINE UREA DERIVATIVES
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Page/Page column 18, (2009/01/20)
The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment
THERAPEUTIC PYRAZOLOQUINOLINE DERIVATIVES
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Page/Page column 42, (2009/01/20)
The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
High affinity central benzodiazepine receptor ligands. Part 2: Quantitative structure-activity relationships and comparative molecular field analysis of pyrazolo[4,3-c]quinolin-3-ones
Savini,Chiasserini,Pellerano,Biggio,Maciocco,Serra,Cinone,Carrieri,Altomare,Carotti
, p. 431 - 444 (2007/10/03)
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 recepto
High affinity central benzodiazepine receptor ligands: Synthesis and structure-activity relationship studies of a new series of pyrazolo[4,3- c]quinolin-3-ones
Savini,Massarelli,Nencini,Pellerano,Biggio,Maciocco,Tuligi,Carrieri,Cinone,Carotti
, p. 389 - 399 (2007/10/03)
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.
