Synthesis and Sar of 1-Hydroxy-1h-benzo[d] Imidazol-2(3h)-Ones As Inhibitors of Damino Acid Oxidase
ACS medicinal chemistry letters(2012)
摘要
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). Inhibitory potency is largely dependent on the size and position of substituents on the benzene ring with IC(50) values of the compounds ranging from 70 nM to greater than 100 µM. 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. Some of these compounds were given to mice orally together with D-serine to assess their effects on plasma D-serine pharmacokinetics.
更多查看译文
关键词
D-amino acid oxidase (DAAO),D-serine,NMDA receptors,glucuronidation
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要