| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370830 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
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]quinazoline, 42 (PDE10A IC50 = 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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jan Kehler, Andreas Ritzen, Morten Langgård, Sebastian Leth Petersen, Mohamed M. Farah, Christoffer Bundgaard, Claus Tornby Christoffersen, Jacob Nielsen, John Paul Kilburn,