Synthesis and biological evaluation of ticagrelor derivatives as novel antiplatelet agents

H Zhang, J Liu, L Zhang, L Kong, H Yao…

文献索引：Zhang, Hao; Liu, Jun; Zhang, Luyong; Kong, Lingyi; Yao, Hequan; Sun, Hongbin Bioorganic and Medicinal Chemistry Letters, 2012 ,  vol. 22,  # 11  p. 3598 - 3602

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被引用次数: 18

摘要

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 ...