Design and synthesis of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors

被引：25
|
作者：
Song, Bo [1 ]
Xiao, Tong [1 ]
Qi, Xiaolu [1 ]
Li, Ling-Na [1 ]
Qin, Kuiyou [1 ]
Nian, Siyun [1 ]
Hu, Guo-Xin [1 ]
Yu, Yinfei [2 ]
Liang, Guang [1 ,3 ]
Ye, Faqing [1 ,3 ]
机构：
[1] Wenzhou Med Coll, Sch Pharm, Wenzhou 325000, Peoples R China
[2] Wenzhou Med Coll, Affiliated Eye Hosp, Wenzhou 325000, Peoples R China
[3] Wenzhou Med Coll, Bioorgan & Med Chem Res Ctr, Wenzhou 325000, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 04期
关键词：
Monoamine oxidase-B inhibitors; Xanthine derivative; Parkinson's disease; Neuroportective effect; Inhibitory effect;
D O I：
10.1016/j.bmcl.2011.12.094
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Monoamine oxidase-B (MAO-B) inhibitor has been used as neuroprotectants to treat the motor deficits of Parkinson's disease (PD). We designed and synthesized a class of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors. The compounds have various inhibitory effects, with compound 6a having a K-i value of 0.26 mu M. Their promising activity in vitro suggests potential use in the treatment of PD. (C) 2012 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1739 / 1742
页数：4
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