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Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors |
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| Authors: | Asproni Battistina Murineddu Gabriele Pau Amedeo Pinna Gérard A Langgård Morten Christoffersen Claus Tornby Nielsen Jacob Kehler Jan |
| Affiliation: | a Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, Via F. Muroni 23/a, 07100 Sassari, Italy b H. Lundbeck A/S, Department of Medicinal Chemistry, 9 Ottiliavej, DK-2500 Valby, Denmark c H. Lundbeck A/S, Department of Molecular Pharmacology, 9 Ottiliavej, DK-2500 Valby, Denmark d H. Lundbeck A/S, Department of Molecular Neurobiology, 9 Ottiliavej, DK-2500 Valby, Denmark |
| 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 (IC50 = 16 nM). |
| Keywords: | PDE10A inhibition Phenylimidazole-pyrazolo[1,5-c]quinazolines Structure-activity relationships |
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