Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
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Kehler J, Ritzen A, Langgard M, Petersen SL, Farah MM, Bundgaard C, Christoffersen CT, Nielsen J, Kilburn JP
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
Bioorg Med Chem Lett. 2011 Jun 15;21(12):3738-42. doi: 10.1016/j.bmcl.2011.04.067. Epub 2011 Apr 30.
- PubMed ID
- 21602043 [ View in PubMed]
- Abstract
Novel triazoloquinazolines have been found as phosphodiesterase 10A (PDE10A) inhibitors. Structure-activity studies improved the initial micromolar potency which was found in the lead compound by a 100-fold identifying 5-(1H-benzoimidazol-2-ylmethylsulfanyl)-2-methyl-[1,2,4]triazolo[1,5-c]quinazolin e, 42 (PDE10A IC(50)=12 nM) as the most potent compound from the series. Two X-ray structures revealed novel binding modes to the catalytic site of the PDE10A enzyme.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mardepodect cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A IC 50 (nM) 2.6 N/A N/A Details Papaverine cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A IC 50 (nM) 210 N/A N/A Details PQ-10 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A IC 50 (nM) 64 N/A N/A Details