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Bioorg Med Chem. 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.

Author information

1
Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, Via F. Muroni 23/a, 07100 Sassari, Italy. asproni@uniss.it

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).

PMID:
21087867
DOI:
10.1016/j.bmc.2010.10.038
[Indexed for MEDLINE]

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