Design, synthesis, and vasorelaxation activity of novel imperatorin derivatives

Abstract

In this study, a series of novel imperatorin derivatives 7a–7e were designed and synthesized. Their vasorelaxation activities were evaluated by the pharmacological experiments in vitro. Most of the tested compounds exhibited better water solubility and vasorelaxation activity in different degrees, especially 7b and 7c with EC₅₀ values of 2.29 and 2.63 μM, respectively on mesenteric artery, 7d and 7e with EC₅₀ values of 1.04 and 2.65 μM, respectively on brain artery. The results indicated that these novel compounds have a potential interest for the development of novel and potent vasorelaxant agents for different kinds of arteries.

Keywords:

• hypertension
• imperatorin
• xanthotoxol
• vasorelaxation activity
• synthesis

Acknowledgments

This work was financially supported by the National Natural Science Foundation of China (Nos 81202494, 30730110). We are grateful to Prof. Zongru Guo for practical guidance during the course of this project.