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Synthesis of a Novel Series of Amino Acid Prodrugs Based on Thienopyridine Scaffolds and Evaluation of Their Antiplatelet Activity.

ABSTRACT: The thienopyridines class of drugs used as P2Y₁₂ 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.

SUBMITTER: Lu N

PROVIDER: S-EPMC6102589 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature

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Synthesis of a Novel Series of Amino Acid Prodrugs Based on Thienopyridine Scaffolds and Evaluation of Their Antiplatelet Activity.

Lu Nan N Li Lingjun L Zheng Xuemin X Zhang Shijun S Li Yuquan Y Yuan Jing J Wei Qunchao Q Xu Youjun Y Meng Fancui F

Molecules (Basel, Switzerland) 20180428 5

The thienopyridines class of drugs used as P2Y<sub>12</sub> 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 ED<sub>50</sub> and bleeding time of the most potent compounds were compared with commercial drugs. The results showed c ...[more]

PMID: 29710801

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