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

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Asproni B, Murineddu G, Pau A, Pinna GA, Langgard M, Christoffersen CT, Nielsen J, Kehler J

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

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

PubMed ID

21087867 [ View in PubMed

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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]quinaz oline (1q) showed the highest affinity for PDE10A enzyme (IC(50)=16nM).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Papaverine	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	IC 50 (nM)	17	N/A	N/A	Details