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ID: ALA1641409

Journal: Bioorg Med Chem

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

Authors: Asproni B, Murineddu G, Pau A, Pinna GA, Langgård M, Christoffersen CT, Nielsen J, Kehler J.

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

CiteXplore: 21087867

DOI: 10.1016/j.bmc.2010.10.038