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Synthesis of a Novel Series of Amino Acid Prodrugs Based on Thienopyridine Scaffolds and Evaluation of Their Antiplatelet Activity
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Synthesis of a Novel Series of Amino Acid Prodrugs Based on Thienopyridine Scaffolds and Evaluation of Their Antiplatelet Activity
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Journal Article
Synthesis of a Novel Series of Amino Acid Prodrugs Based on Thienopyridine Scaffolds and Evaluation of Their Antiplatelet Activity
2018
Overview
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.
Publisher
MDPI AG,MDPI
Subject
/ Adenosine Diphosphate - adverse effects
/ Animals
/ Dose-Response Relationship, Drug
/ Drugs
/ Enzymes
/ Male
/ Platelet Aggregation - drug effects
/ Prasugrel Hydrochloride - administration & dosage
/ Prasugrel Hydrochloride - pharmacology
/ Prodrugs - administration & dosage
/ Prodrugs - chemical synthesis
/ Rats
/ Ticlopidine - administration & dosage
