1159706-33-8Relevant articles and documents
HYDROXYQUINOLIN-2(1H)-ONES AND DERIVATIVES THEREOF
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Page/Page column 63, (2010/07/10)
This invention relates to known and novel hydroxyquinolin-2(1H)-ones and derivatives thereof which are useful for the treatment of cognitive-related disorders and neuropathic pain disorders in a mammal, e.g., a human. The invention also relates to pharmaceutical compositions containing such compounds.
Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors
Duplantier, Allen J.,Becker, Stacey L.,Bohanon, Michael J.,Borzilleri, Kris A.,Chrunyk, Boris A.,Downs, James T.,Hu, Lain-Yen,El-Kattan, Ayman,James, Larry C.,Liu, Shenping,Lu, Jiemin,Maklad, Noha,Mansour, Mahmoud N.,Mente, Scot,Piotrowski, Mary A.,Sakya, Subas M.,Sheehan, Susan,Steyn, Stefanus J.,Strick, Christine A.,Williams, Victoria A.,Zhang, Lei
experimental part, p. 3576 - 3585 (2010/03/30)
3-Hydroxyquinolin-2(1H)-one (2) was discovered by high throughput screening in a functional assay to be a potent inhibitor of human DAAO, and its binding affinity was confirmed in a Biacore assay. Cocrystallization of 2 with the human DAAO enzyme defined