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

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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DOI: 10.1016/j.bmc.2010.10.038

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).

Item Type:	Article
ID Code:	5490
Status:	Published
Refereed:	Yes
Uncontrolled Keywords:	PDE10A inhibition, phenylimidazole-pyrazolo[1,5-c]quinazolines, structure–activity relationships
Subjects:	Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:	001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:	Pergamon-Elsevier Science
eISSN:	1464-3391
Copyright Holders:	© 2010 Elsevier
Deposited On:	04 Mar 2011 16:15

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