Key result
Novel trimethylpyrazine-2-carbonyloxy-cinnamic acids exhibited high in vitro activity, with compound F'10 showing potent protection against oxidative damage and F3 demonstrating anti-platelet activity.
Effect estimate: EC50 = 1.7 μM (F'10); IC50 = 9.6 μM (F3)
Novel trimethylpyrazine-2-carbonyloxy-cinnamic acids demonstrate potent in vitro anti-platelet and antioxidant properties, highlighting their potential for future cardiovascular drug development.
These compounds require extensive preclinical and clinical validation before consideration; leaves open their therapeutic role in cardiovascular disease.
A series of novel trimethylpyrazine-2-carbonyloxy-cinnamic acids and esters were designed, synthesized and evaluated for their inhibitory effect on adenosine diphosphate (ADP)-induced platelet aggregation in vitro and also assayed for their protective effect against hydrogen peroxide (H2O2)-induced oxidative damage on Ea.hy926 cells. The results showed that many compounds exhibited high activity in one or both of the assays, of which, compound F′10 displayed the highest protective effect on the proliferation of the damaged Ea.hy926 cells (EC50 = 1.7 μM), presenting almost 40 times higher potency than that of lipoic acid, and compound F3 was the most active anti-platelet aggregation agent with IC50 = 9.6 μM, comparable to that of clopidogrel. The structure–activity relationships of these compounds were also discussed.
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Chen et al. (2014) studied Oxidative damage and platelet aggregation. Trimethylpyrazine-2-carbonyloxy-cinnamic acids and esters vs. Lipoic acid and clopidogrel was evaluated on Inhibitory effect on ADP-induced platelet aggregation and protective effect against H2O2-induced oxidative damage on Ea.hy926 cells (EC50 = 1.7 μM (F'10); IC50 = 9.6 μM (F3)). Novel trimethylpyrazine-2-carbonyloxy-cinnamic acids exhibited high in vitro activity, with compound F'10 showing potent protection against oxidative damage and F3 demonstrating anti-platelet activity.
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