1H-NMR、13C-NMR及MS確證?;钚詼y試結(jié)果表明,化合物5h、5b的活性強于陽性對照藥奧扎格雷鈉,具有抗血小板聚集活性。結(jié)論 4-甲基-(3'S, 4'S)-凱林硫代內(nèi)酯衍生物具有良好的抗血小板聚集活性,值得進一步研究。;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 by 1H-NMR, 13C-NMR, and MS data. The in vitro assay indicated that compounds 5h and 5b exhibited remarkable anti-platelet aggregation activities, and they were better than control drug ozagrel sodium. Conclusion 4-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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首頁 > 過刊瀏覽>2015年第30卷第9期 >2015,30(9):1051-1056. DOI:10.7501/j.issn.1674-5515.2015.09.001
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4-甲基-(3'S, 4'S)-凱林硫代內(nèi)酯衍生物的合成及其體外抗血小板聚集活性研究

Synthesis of 4-methyl-(3'S, 4'S)-khelthiolactone derivatives and their anti-platelet aggregation activities in vitro

發(fā)布日期:2015-09-24