- New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies
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This paper reports the study of some 2-arylpyrazolo[3,4-c]quinolin-4-ones, 4-amines, and 4-amino-substituted derivatives designed as human A3 adenosine receptor (AR) antagonists. Most of the herein reported compounds showed a nanomolar affinity
- Colotta, Vittoria,Catarzi, Daniela,Varano, Flavia,Capelli, Francesca,Lenzi, Ombretta,Filacchioni, Guido,Martini, Claudia,Trincavelli, Letizia,Ciampi, Osele,Pugliese, Anna Maria,Pedata, Felicita,Schiesaro, Andrea,Morizzo, Erika,Moro, Stefano
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p. 4061 - 4074
(2008/02/12)
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- Tricyclic heteroaromatic systems. Pyrazolo[3,4-c]quinolin-4-ones and pyrazolo[3,4-c]quinoline-1,4-diones: Synthesis and benzodiazepine receptor activity
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Some pyrazolo[3,4-c]quinoline-4-ones 1-14 and pyrazolo[3,4-c]-quinoline-1,4-diones 15-17 were prepared and biologically evaluated for their binding at the benzodiazepine receptor (BZR) in rat cortical membranes. The moderate binding activity of 1-5, 7, 9-10, 13 is attributable to the lack of the optional proton acceptor at position-1, while the inactivity of the 1,4-dione derivatives 15-17 is due to the lack of the essential proton acceptor at position-3. These conclusions confirm the validity of our proposed pharmacophoric model.
- Catarzi, Daniela,Colotta, Vittoria,Varano, Flavia,Cecchi, Lucia,Filacchioni, Guido,Galli, Alessandro,Costagli, Chiara
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p. 383 - 386
(2007/10/03)
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