Jump to main content
Jump to site search

Issue 31, 2014
Previous Article Next Article

Design, synthesis and biological evaluation of hydrogen sulfide releasing derivatives of 3-n-butylphthalide as potential antiplatelet and antithrombotic agents

Author affiliations

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.

Graphical abstract: Design, synthesis and biological evaluation of hydrogen sulfide releasing derivatives of 3-n-butylphthalide as potential antiplatelet and antithrombotic agents

Back to tab navigation

Supplementary files

Article information


Submitted
22 Apr 2014
Accepted
19 Jun 2014
First published
20 Jun 2014

Org. Biomol. Chem., 2014,12, 5995-6004
Article type
Paper
Author version available

Design, synthesis and biological evaluation of hydrogen sulfide releasing derivatives of 3-n-butylphthalide as potential antiplatelet and antithrombotic agents

X. Wang, L. Wang, X. Sheng, Z. Huang, T. Li, M. Zhang, J. Xu, H. Ji, J. Yin and Y. Zhang, Org. Biomol. Chem., 2014, 12, 5995
DOI: 10.1039/C4OB00830H

Social activity

Search articles by author

Spotlight

Advertisements