Medicinal Chemistry

Design, synthesis and preliminary evaluation of novel imperatorin derivatives as vasorelaxant agents

N Li, J He, Y Zhan, N Zhou, J Zhang

Index: Li, Na; He, Jianyu; Zhan, Yingzhuan; Zhou, Nan; Zhang, Jie Medicinal Chemistry, 2011 , vol. 7, # 1 p. 18 - 23

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Citation Number: 10

Abstract

A series of novel imperatorin derivatives were synthesized from commercially available xanthotoxin. The in vitro pharmacological evaluation indicated that all of the compounds possessed potent vasodilatory activity. Among them, compounds (5b),(5d) and (5e) exhibited higher vasdilatory activity (with EC50 values of 0.68 μM, 0.59 μM and 0.49 μM, respectively) than imperatorin (EC50= 1.12 μM). The program Volsurf was used to predict ...

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