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GAO Yang, YIN Wei, LIU Jingchao, KANG Fenghua, JIAN Yanlin, ZHOU Jinpei, HUANG Zhangjian, ZHANG Yihua. Design, synthesis and antiplatelet evaluation of tetramethylpyrazine/chalcone hybrids[J]. Journal of China Pharmaceutical University, 2017, 48(1): 23-30. DOI: 10.11665/j.issn.1000-5048.20170104
Citation: GAO Yang, YIN Wei, LIU Jingchao, KANG Fenghua, JIAN Yanlin, ZHOU Jinpei, HUANG Zhangjian, ZHANG Yihua. Design, synthesis and antiplatelet evaluation of tetramethylpyrazine/chalcone hybrids[J]. Journal of China Pharmaceutical University, 2017, 48(1): 23-30. DOI: 10.11665/j.issn.1000-5048.20170104
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Design, synthesis and antiplatelet evaluation of tetramethylpyrazine/chalcone hybrids

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  • In order to search for new antiplatelet agents with higher potency, a series of tetramethylpyrazine(TMP)/chalcone hybrids( 2 - 26 )were synthesized and evaluated based on the principle of bioisostere and hybridization. They exerted inhibitory activity against adenosine diphosphate(ADP)-induced and arachidonic acid(AA)-induced platelet aggregation to varied extent. Among them, compound 8 was the most potent with IC50 of 0. 14 mmol/L on ADP-induced platelet aggregation(9. 1 folds of TMP and 10. 5 folds of chalcone)and 0. 09 mmol/L on AA-induced platelet aggregation(8. 8 folds of TMP and 10. 0 folds of chalcone), which was superior to clinically used anti-platelet drug aspirin(ASP, IC50=0. 15 mmol/L).
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