Synthesis and biological evaluation of nitric oxide releasing derivatives of 6-amino-3-n-butylphthalide as potential antiplatelet agents

被引：43

作者：

Wang, Xiaoli ^{[1
,2
]}

Wang, Linna ^{[1
,3
]}

Huang, Zhangjian ^{[1
,2
]}

Sheng, Xiao ^{[1
,2
]}

Li, Tingting ^{[1
,3
]}

Ji, Hui ^{[1
,3
]}

Xu, Jinyi ^{[1
,2
]}

Zhang, Yihua ^{[1
,2
]}

机构：

[1] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Peoples R China

[2] China Pharmaceut Univ, Ctr Drug Discovery, Nanjing 210009, Peoples R China

[3] China Pharmaceut Univ, Dept Pharmacol, Nanjing 210009, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 07期

关键词：

3-n-Butylphthalide (NBP); 6-Amino-3-n-butylphthalide; NO-releasing derivatives; Antiplatelet agents; Ischemic stroke; STROKE; DRUGS;

D O I：

10.1016/j.bmcl.2013.02.035

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel nitric oxide releasing derivatives of 6-amino-3-n-butylphthalide were designed, synthesized and evaluated as potential antiplatelet agents. Compound 10b significantly inhibited the adenosine diphosphate (ADP)-induced platelet aggregation in vitro, superior to 6-amino-3-n-butylphthalide, 3-n-butylphthalide (NBP) and ticlopidine. Meanwhile 10b released moderate levels of NO, which could be beneficial for improving cardiovascular and cerebral circulation. Furthermore, 10b had an enhanced aqueous solubility relative to NBP. These findings may provide new insights into the development of novel antiplatelet agents for the treatment of thrombosis-related ischemic stroke. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：1985 / 1988

页数：4

共 17 条

[1] Carbonic anhydrase inhibitors: Water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects [J].