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Synthesis of 4-methyl-(3′S, 4′S)-khelthiolactone derivatives and their anti-platelet aggregation activitiesin vitro
Pages: 1051-1056
Year: Issue:  9
Journal: World Phytomedicines

Keyword:  khelthiolactone7-hydroxy-4-methyl coumarinozagrel sodiumsynthesisanti-platelet aggregation activity;
Abstract: Objective To design and synthesize khelthiolactone derivatives, and to evaluate their anti-platelet aggregation activities in virto. Methods 7-Hydroxy-4-methyl coumarin was used as starting material to synthesize the target compounds by nucleophilic substitution reaction, claisen rearrangement, sulfuration reaction, sharpless asymmetrical dihydroxylation, and esterification reactions. The anti-platelet aggregation activities of the synthesized compounds were evaluated by microplate reader method.Results Eight novel khelthiolactone derivatives were synthesized and characterized by1H-NMR,13C-NMR, and MS data. Thein vitro assay indicated that compounds 5h and5b exhibited remarkable anti-platelet aggregation activities, and they were better than control drug ozagrel sodium.Conclusion4-Methyl-(3′S, 4′S)-khelthiolactone derivatives have good anti-platelet aggregation activities, which could be a valuable candidate for further development.
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