Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5- c ]quinazolines as potent phosphodiesterase 10A inhibitors

作者: Battistina Asproni , Gabriele Murineddu , Amedeo Pau , Gérard A. Pinna , Morten Langgård

DOI: 10.1016/J.BMC.2010.10.038

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摘要: Abstract A series of phenylimidazole-pyrazolo[1,5- c ]quinazolines 1a – q was designed, synthesized and characterised as a novel class potent phophodiesterase 10A (PDE10A) inhibitors. In this series, 2,9-dimethyl-5-(2-(1-methyl-4-phenyl-1 H -imidazol-2-yl)ethyl)pyrazolo[1,5- ]quinazoline ( 1q ) showed the highest affinity for PDE10A enzyme (IC 50  = 16 nM).

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