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Updated: May 22, 2026

Microfluidics in Assessing Platelet Function
Published on: November 8, 2024
Synthesis and biological evaluation of ticagrelor derivatives as novel antiplatelet agents
Hao Zhang1, Jun Liu, Luyong Zhang
1Center of Drug Discovery, College of Pharmacy, China Pharmaceutical University, Nanjing, China.
Abstract:
Ticagrelor (1) is the first reversible P2Y12 receptor antagonist blocking adenine diphosphate (ADP)-induced platelet aggregation with rapid onset and offset of effects. In this study, synthesis of ticagrelor and its derivatives has been accomplished in a convergent way. The compound design was based on modifications of ticagrelor and its major metabolite (33) in order to ameliorate their pharmacokinetic properties and dosing profile. The final compounds (1a-g, 35a-g) were evaluated for their inhibitory effect on ADP-induced platelet aggregation in rats. The assay results showed that some compounds (e.g., 1b, 1d, 33, 35b, 35f) exhibited comparable potency with that of ticagrelor.
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