Document Report Card
Basic Information
ID: ALA1777757
Journal: Bioorg Med Chem Lett
Title: Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
Authors: Kehler J, Ritzen A, Langgård M, Petersen SL, Farah MM, Bundgaard C, Christoffersen CT, Nielsen J, Kilburn JP.
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 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.
CiteXplore: 21602043