Citation: Fan Lingling, Li Yi, Luo Bilan, Fan Judi, Li yong, Tang Lei. Syntheses and Anti-Platelet Aggregations Activity Evaluations of Pyrazines[J]. Chemistry, ;2019, 82(2): 128-132. shu

Syntheses and Anti-Platelet Aggregations Activity Evaluations of Pyrazines

College of Pharmacy, Guizhou Medical University, Guiyang 550025

Corresponding author: Tang Lei, 2317972657@qq.com
Received Date: 10 September 2018
Accepted Date: 5 October 2018

Figures(5)

In order to improve the antiplatelet agglutination activity of ligustrazine, different diamines, 2, 3-butanedione and lipoic acid were used as starting materials, seven ligustrazine derivatives were synthesized via four routes, including bromination, hydrolysis, cyclization, oxidation, hydrogenation and substitution reaction. Their structures were confirmed by ¹H NMR, ¹³C NMR and ESI-MS, and the in vitro anti-platelet aggregation activities were tested preliminarily by the Born turbidimetric method. The experimental results showed that compounds 1 (IC₅₀=0.26 mmol/L), 2 (IC₅₀=0.27 mmol/L) and 7 (IC₅₀=0.21 mmol/L) exhibit significant inhibitory activity for adenosine diphosphate (ADP) induced platelet aggregation, which are superior to the lead compound ligustrazine (IC₅₀=0.49 mmol/L). Therefore, without changing ligustrazine pharmacophore, cyclization in different degree can obviously improve the antiplatelet agglutination activity of ligustrazine, which has useful reference value for the structure modification of lead compound.
- Ligustrazine derivatives,
- Design,
- Synthesis,
- Anti-platelet aggregation activity
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