Design, synthesis and antiplatelet evaluation of tetramethylpyrazine/chalcone hybrids
10.11665/j.issn.1000-5048.20170104
- VernacularTitle:川芎嗪/查耳酮类杂合物的设计、合成及抗血小板聚集活性
- Author:
Yang GAO
;
Wei YIN
;
Jingchao LIU
;
Fenghua KANG
;
Yanlin JIAN
;
Jinpei ZHOU
;
Zhangjian HUANG
;
Yihua ZHANG
- Keywords:
tetramethylpyrazine;
chalcone;
hybridization;
aspirin;
antiplatelet;
synthesis
- From:
Journal of China Pharmaceutical University
2017;48(1):23-30
- CountryChina
- Language:Chinese
-
Abstract:
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 hybrid-ization. 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) .
