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Design, Synthesis and Biological Evaluation of Hydrogen Sulfide Releasing Derivatives of 3-n-butylphthalide as Potential Antiplatelet and Antithrombotic Agents

Design, Synthesis and Biological Evaluation of Hydrogen Sulfide Releasing Derivatives of 3-n-butylphthalide as Potential Antiplatelet and Antithrombotic Agents

Xiaoli Wang, Linna Wang, Xiao Sheng, Zhangjian Huang, Tingting Li, Ming Zhang, Jinyi Xu, Hui Ji, Jian Yin, Yihua Zhang

Org Biomol Chem. 2014 Aug 21;12(31):5995-6004.

PMID: 24988475

Abstract:

In the present study, a series of hydrogen sulfide (H2S) releasing derivatives (8a-g and 9a-f) of 3-n-butylphthalide (NBP) were designed, synthesized and biologically evaluated. The most promising compound 8e significantly inhibited the adenosine diphosphate (ADP) and arachidonic acid (AA)-induced platelet aggregation in vitro, superior to NBP, ticlopidine hydrochloride and aspirin. Furthermore, 8e could slowly produce moderate levels of H2S in vitro, which could be beneficial for improving cardiovascular and cerebral circulation. Most importantly, 8e protected against the collagen and adrenaline induced thrombosis in mice, and exhibited greater antithrombotic activity than NBP and aspirin in rats. Overall, 8e could warrant further investigation for the treatment of thrombosis-related ischemic stroke.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP68559604	Ticlopidine Related Compound A		68559-60-4	Price

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