title: Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
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.
authors: H. Lundbeck A/S, Department of Discovery Chemistry & DMPK, Valby, Denmark. jke@lundbeck.com
authors: Jan
authors: J
authors: Kehler
authors: Andreas
authors: A
authors: Ritzen
authors: Morten
authors: M
authors: Langgård
authors: Sebastian Leth
authors: SL
authors: Petersen
authors: Mohamed M
authors: MM
authors: Farah
authors: Christoffer
authors: C
authors: Bundgaard
authors: Claus Tornby
authors: CT
authors: Christoffersen
authors: Jacob
authors: J
authors: Nielsen
authors: John Paul
authors: JP
authors: Kilburn