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.

Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo [1,5-a]pyrimidine Derivatives.3. New 6-(3-Thienyl) Series as a1 Selective Ligands / S. SELLERI; F. BRUNI; C. COSTAGLI; A. COSTANZO; G. GUERRINI; G. CICIANI; P.GRATTERI; C.BONACCINI; P.MALMBERG AIELLO; F.BESNARD; S.RENARD; B. COSTA; C. MARTINI. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 46:(2003), pp. 310-313. [10.1021/jm020999w]

Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo [1,5-a]pyrimidine Derivatives.3. New 6-(3-Thienyl) Series as a1 Selective Ligands

SELLERI, SILVIA;BRUNI, FABRIZIO;COSTANZO, ANNARELLA;GUERRINI, GABRIELLA;CICIANI, GIOVANNA;GRATTERI, PAOLA;MALMBERG, PETRA;
2003

Abstract

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.
2003
46
310
313
S. SELLERI; F. BRUNI; C. COSTAGLI; A. COSTANZO; G. GUERRINI; G. CICIANI; P.GRATTERI; C.BONACCINI; P.MALMBERG AIELLO; F.BESNARD; S.RENARD; B. COSTA; C....espandi
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/310047
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