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Bioorg Med Chem Lett. 2011 Jun 15;21(12):3738-42. doi: 10.1016/j.bmcl.2011.04.067. Epub 2011 Apr 30.

Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.

Author information

1
H. Lundbeck A/S, Department of Discovery Chemistry & DMPK, Valby, Denmark. jke@lundbeck.com

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.

PMID:
21602043
DOI:
10.1016/j.bmcl.2011.04.067
[Indexed for MEDLINE]

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