Structural highlights
Publication Abstract from PubMed
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]qui nazoline, 42 (PDE10A IC(50)=12nM) as the most potent compound from the series. Two X-ray structures revealed novel binding modes to the catalytic site of the PDE10A enzyme.
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.,Kehler J, Ritzen A, Langgard M, Petersen SL, Farah MM, Bundgaard C, Christoffersen CT, Nielsen J, Kilburn JP Bioorg Med Chem Lett. 2011 Jun 15;21(12):3738-42. Epub 2011 Apr 30. PMID:21602043[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ 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. Epub 2011 Apr 30. PMID:21602043 doi:10.1016/j.bmcl.2011.04.067
