期刊
MOLECULES
卷 23, 期 5, 页码 -出版社
MDPI
DOI: 10.3390/molecules23051041
关键词
thienopyridines; P2Y(12) receptor antagonist; antiplatelet; amino acid prodrugs; ADP-induced platelet aggregation
资金
- Tianjin Natural Science Foundation-Young Foundation [17JCQNJC13700, 17JCQNJC13100]
- Innovative Research Team in SYPHU by Chinese Central Government [51150039]
The thienopyridines class of drugs used as P2Y(12) receptor antagonists plays a vital role in antiplatelet therapy. To further optimized this compound class, we designed and synthesized a series of amino acid prodrugs of 2-hydroxytetrahydrothienopyridine. All compounds were then evaluated for their inhibitory effect on ADP-induced platelet aggregation in rats and then ED50 and bleeding time of the most potent compounds were compared with commercial drugs. The results showed compound 5c could be a potent and safe candidate for further research.
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