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Citation: . Syntheses and Anti-Platelet Aggregation Activities Evaluation of Ligustrazine Derivatives[J]. Chemistry, ;2018, 81(6): 543-547. shu

Syntheses and Anti-Platelet Aggregation Activities Evaluation of Ligustrazine Derivatives

Received Date: 8 December 2017
Accepted Date: 17 April 2018

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Using ligustrazine (TMP) and o-phenylenediamine as raw materials, seven derivatives were synthesized via KMnO₄ oxidation, esterification, cyclization and reduction. The structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. The in vitro anti-platelet aggregation activities of the target compounds have been preliminarily tested by the Born turbidimetric method, and the experimental results showed that compounds 3 (IC₅₀=0.23mmol/L) and 7 (IC₅₀=0.27mmol/L) have significant inhibitory activity for adenosine diphosphate (ADP) induced platelet aggregation, higher than that of ligustrazine (IC₅₀=0.42 mmol/L).
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