期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 3, 期 10, 页码 839-843出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml300212a
关键词
D-amino acid oxidase (DAAO); D-serine; NMDA receptors; glucuronidation
资金
- National Institutes of Health [R01MH091387]
- Johns Hopkins Brain Science Institute NeuroTranslational Drug Discovery program
A series of 1-hydroxy-1H-benzo[d]imidazol-2(3H)-ones were synthesized and evaluated for their ability to inhibit human and porcine forms of D-amino acid oxidase (DAAO). The inhibitory potency is largely dependent on the size and position of substituents on the benzene ring with IC50 values of the compounds ranging from 70 nM to greater than 100 mu M. Structure-activity relationships of this new class of DAAO inhibitors will be presented in detail along with comparisons to previously published SAR data from other classes of DAAO inhibitors. Two of these compounds were given to mice orally together with D-serine to assess their effects on plasma D-serine pharmacokinetics.
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