Issue 16, 2011
From the journal:

Organic & Biomolecular Chemistry

Design, synthesis and evaluation of nitric oxide releasing derivatives of 3-n-butylphthalide as antiplatelet and antithrombotic agents†

Xuliang Wang,a   Yang Li,a   Qian Zhao,b   Zhenli Min,a   Chao Zhang,b   Yisheng Lai,a   Hui Ji,*b   Sixun Penga  and  Yihua Zhang*a  

* Corresponding authors

a Center of Drug Discovery, China Pharmaceutical University, Nanjing, P. R. China
E-mail: zyhtgd@sohu.com
Fax: +86-25-83271015
Tel: +86-25-83271015

b Department of Pharmacology, China Pharmaceutical University, Nanjing, P. R. China
E-mail: huijicpu@163.com
Fax: +86-25-86021369
Tel: +86-25-86021369

Abstract

Novel nitric oxide (NO) releasing derivatives (7a–7l) of 3-n-butylphthalide (NBP) were designed and synthesized. Compound 7e inhibited the adenosine diphosphate (ADP), thrombin (TH) and arachidonic acid (AA)-induced in vitroplatelet aggregation, superior to NBP and aspirin, released moderate levels of NO, and improved aqueous solubility relative to NBP. Furthermore, 7e exhibited greater antithrombotic activity than NBP and aspirin in rats, and protected against collagen and adrenaline-induced thrombosis in mice. Therefore, NO-releasing NBP derivatives possessed potent antiplatelet aggregation and antithrombotic activity. Our findings may aid in the design of new therapeutic agents for the treatment of thrombosis-related ischemic stroke.

Graphical abstract: Design, synthesis and evaluation of nitric oxide releasing derivatives of 3-n-butylphthalide as antiplatelet and antithrombotic agents

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Article information

DOI
https://doi.org/10.1039/C1OB05478C
Article type
Paper
Submitted
26 Mar 2011
Accepted
12 Apr 2011
First published
12 Apr 2011

Org. Biomol. Chem., 2011,9, 5670-5681

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Design, synthesis and evaluation of nitric oxide releasing derivatives of 3-n-butylphthalide as antiplatelet and antithrombotic agents

X. Wang, Y. Li, Q. Zhao, Z. Min, C. Zhang, Y. Lai, H. Ji, S. Peng and Y. Zhang, Org. Biomol. Chem., 2011, 9, 5670 DOI: 10.1039/C1OB05478C

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