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Updated: Aug 1, 2025

Platelet-based Detection of Nitric Oxide in Blood by Measuring VASP Phosphorylation
Published on: January 7, 2019
Synthesis and Evaluation of Novel Nitric Oxide-Donating Ligustrazine Derivatives as Potent Antiplatelet Aggregation
Han-Xu Li1, Jian-Hui Tian1, Hua-Yu Li1
1Institute of Pharmaceutical Process, Hubei Province Key Laboratory of Occupationl Hazard Identification and Control, School of Medicine, Wuhan University of Science and Technology, Wuhan 430065, China.
Abstract:
Antiplatelet aggregation agents have demonstrated clinical benefits in the treatment of ischemic stroke. In our study, a series of novel nitric oxide (NO)-donating ligustrazine derivatives were designed and synthesized as antiplatelet aggregation agents. They were evaluated for the inhibitory effect on 5'-diphosphate (ADP)-induced and arachidonic acid (AA)-induced platelet aggregation in vitro. The results showed that compound 15d displayed the best activity in both ADP-induced and AA-induced assays, and compound 14a also showed quite better activity than ligustrazine. The preliminary structure-activity relationships of these novel NO-donating ligustrazine derivatives were discussed. Moreover, these compounds were docked with the thromboxane A2 receptor to study the structure-activity relationships. These results suggested that the novel NO-donating ligustrazine derivatives 14a and 15d deserve further study as potent antiplatelet aggregation agents.
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