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]
- 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).
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- 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