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Bioorg. Med. Chem. Lett. · Jun 2012
Synthesis and biological evaluation of ticagrelor derivatives as novel antiplatelet agents.
- Hao Zhang, Jun Liu, Luyong Zhang, Lingyi Kong, Hequan Yao, and Hongbin Sun.
- Center of Drug Discovery, College of Pharmacy, China Pharmaceutical University, Nanjing, China.
- Bioorg. Med. Chem. Lett. 2012 Jun 1;22(11):3598-602.
AbstractTicagrelor (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.Copyright © 2012 Elsevier Ltd. All rights reserved.
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