Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo[1,5-a]pyrimidine Derivatives. 3. New 6-(3-Thienyl) Series as α1 Selective Ligands

Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo[1,5-a]pyrimidine Derivatives. 3. New 6-(3-Thienyl) Series as α1 Selective Ligands

New 3-aryl-6-(3-thienyl)pyrazolo[1,5-a]pyrimidin-7-ones (2a−j) are synthesized and evaluated in vitro on Bz/GABAA receptors and on recombinant benzodiazepine receptors (αxβ2/3γ2; x = 1−3, 5) expressed in HEK293 cells. SAR studies on the new compounds are conducted and molecular modeling is accomplis...

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Veröffentlicht in:Journal of medicinal chemistry 2003-01, Vol.46 (2), p.310-313
Hauptverfasser: Selleri, Silvia, Bruni, Fabrizio, Costagli, Camilla, Costanzo, Annarella, Guerrini, Gabriella, Ciciani, Giovanna, Gratteri, Paola, Bonaccini, Claudia, Malmberg Aiello, Petra, Besnard, François, Renard, Stephane, Costa, Barbara, Martini, Claudia
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
Gabaergic and benzodiazepinic system
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
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Zusammenfassung:New 3-aryl-6-(3-thienyl)pyrazolo[1,5-a]pyrimidin-7-ones (2a−j) are synthesized and evaluated in vitro on Bz/GABAA receptors and on recombinant benzodiazepine receptors (αxβ2/3γ2; x = 1−3, 5) expressed in HEK293 cells. SAR studies on the new compounds are conducted and molecular modeling is accomplished to better investigate requirements leading to subtype selectivity. Some of the synthesized compounds are tested in vivo to explore their pharmacological effect as a consequence of their high α1β2γ2 subtype selectivity observed in vitro.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm020999w