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. 2011 Jan 1;19(1):642-9.
doi: 10.1016/j.bmc.2010.10.038. Epub 2010 Nov 17.

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

Battistina Asproni  1 , Gabriele Murineddu, Amedeo Pau, Gérard A Pinna, Morten Langgård, Claus Tornby Christoffersen, Jacob Nielsen, Jan Kehler
Affiliations

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

Battistina Asproni et al. Bioorg Med Chem. .

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).

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