Synthesis and evaluation of nitric oxide-releasing derivatives of 3-n-butylphthalide as anti-platelet agents

被引:38
作者
Li, Yang [1 ]
Wang, Xuliang [1 ]
Fu, Rong [2 ]
Yu, Wenying [1 ]
Wang, Xiaoli [1 ]
Lai, Yisheng [1 ]
Peng, Sixun [1 ]
Zhang, Yihua [1 ]
机构
[1] China Pharmaceut Univ, Ctr Drug Discovery, Nanjing 210009, Peoples R China
[2] China Pharmaceut Univ, Dept Physiol, Nanjing 210009, Peoples R China
关键词
Ischemic stroke; Thrombus; 3-n-Butylphthalide; Nitric oxide-releasing derivatives; Anti-platelet activity; THROMBUS FORMATION; DONOR; AGGREGATION; STROKE;
D O I
10.1016/j.bmcl.2011.05.082
中图分类号
R914 [药物化学];
学科分类号
100705 [微生物与生化药学];
摘要
Most ischemic stroke results from brain blood vessel blockage by platelet-mediated thrombus, and antiplatelet therapy has been demonstrated clinical benefits in the treatment of this disease. In the present work, novel nitric oxide (NO)-releasing derivatives of an anti-ischemic stroke drug 3-n-butylphthalide (NBP) were synthesized. Compounds 7a and 7c exhibited more potent anti-platelet activity than NBP and aspirin, and released a moderate amount of NO, which is beneficial in improving cardiovascular and cerebral circulation. These findings provide an alternative approach to the development of drugs more potent than NBP for the intervention of ischemic stroke. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4210 / 4214
页数:5
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