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

页码：1739 / 1742

页数：4

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