Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 2, Pages 310-313Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm020999w
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New 3-aryl-6-(3-thienyl)pyrazolo[1,5-alpha]pyrimidin-7-ones (2a-j) are synthesized and evaluated in vitro on Bz/GABA(A) receptors and on recombinant benzodiazepine receptors (alphaxbeta2/3gamma2; 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 alpha1beta2gamma2 subtype selectivity observed in vitro.
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