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Research on the synthesis and vasodilatation activity of imperatorin derivatives

HUANG Limin;LI Youjia;HOU Yajing;WANG Cheng;WEI Di;HE Huaizhen;School of Pharmacy,Xi′an Jiaotong University;The Second Affiliated Hospital of Xi′an Jiaotong University;  
Objective Imperatorin derivatives were designed,synthesized and screened for their vasodilatation activity.Methods 4 imperatorin derivatives were designed and synthesized based on the structure modification of imperatorin.Their vasodilatory activities were screened by multichannel microvascular strain determination method.The interactions between compounds and potential target proteins were analyzed by computer aided drug design software.Results Imperatorin derivatives exhibited different degrees of vasodilatation activity in different blood vessels.Conclusion In this research,the imperatorin derivatives were synthesized by optimizing the Williamson reaction with simple procedure and mild conditions.4 compounds all exhibited certain vasodilatation activity.Among them,compound 5 possessed the best activity.Further molecular docking research also indicated that compound 5 had a better affinity with the potential target proteins.This study provided theoretical basis for optimizing the structure of imperatorin in the future research.
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