Asproni, Battistina and Murineddu, Gabriele and Pau, Amedeo and Pinna, Gérard Aimé and Langgàrd, Morten and Christoffersen, Claus Tornby and Nielsen, Jacob and Kehler, Jan (2011) Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors. Bioorganic & Medicinal Chemistry, Vol. 19 (1), p. 642-649. eISSN 1464-3391. Article.
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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 (IC50 = 16 nM).
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