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

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.
AuthorsXiaoli Wang, Linna Wang, Xiao Sheng, Zhangjian Huang, Tingting Li, Ming Zhang, Jinyi Xu, Hui Ji, Jian Yin, Yihua Zhang
JournalOrganic & biomolecular chemistry (Org Biomol Chem) Vol. 12 Issue 31 Pg. 5995-6004 (Aug 21 2014) ISSN: 1477-0539 [Electronic] England
PMID24988475 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Benzofurans
  • Fibrinolytic Agents
  • Platelet Aggregation Inhibitors
  • Adenosine Diphosphate
  • 3-n-butylphthalide
  • Hydrogen Sulfide
Topics
  • Adenosine Diphosphate (pharmacology)
  • Administration, Oral
  • Animals
  • Benzofurans (administration & dosage, chemical synthesis, chemistry, pharmacology)
  • Drug Design
  • Fibrinolytic Agents (administration & dosage, chemical synthesis, chemistry, pharmacology)
  • Hydrogen Sulfide (metabolism)
  • Inhibitory Concentration 50
  • Male
  • Mice, Inbred ICR
  • Platelet Aggregation (drug effects)
  • Platelet Aggregation Inhibitors (administration & dosage, chemical synthesis, chemistry, pharmacology)
  • Rabbits
  • Rats, Sprague-Dawley
  • Survival Analysis

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