Design, Synthesis and Preliminary Evaluation of Novel Imperatorin Derivatives as Vasorelaxant Agents

Na Li; Jianyu He; Yingzhuan Zhan; Nan Zhou; Jie Zhang

doi:10.2174/157340611794072715

Design, Synthesis and Preliminary Evaluation of Novel Imperatorin Derivatives as Vasorelaxant Agents

Na Li
, Jianyu He
, Yingzhuan Zhan
, Nan Zhou
, Jie Zhang

医学部

Xi'an Jiaotong University

科研成果: 期刊稿件 › 文章 › 同行评审

19 引用（Scopus）

摘要

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 the derivatives' ADMErelevant descriptors. The results suggested that these novel compounds had a potential interest for the development of novel and potent vasorelaxant agents.

源语言	英语
页（从-至）	18-23
页数	6
期刊	Medicinal Chemistry
卷	7
期	1
DOI	https://doi.org/10.2174/157340611794072715
出版状态	已出版 - 1月 2011

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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 the derivatives' ADMErelevant descriptors. The results suggested that these novel compounds had a potential interest for the development of novel and potent vasorelaxant agents.",

keywords = "Hypertension, Imperatorin derivatives, Vasodilatory activity, Vasorelaxant agents",

author = "Na Li and Jianyu He and Yingzhuan Zhan and Nan Zhou and Jie Zhang",

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T1 - Design, Synthesis and Preliminary Evaluation of Novel Imperatorin Derivatives as Vasorelaxant Agents

AU - Li, Na

AU - He, Jianyu

AU - Zhan, Yingzhuan

AU - Zhou, Nan

AU - Zhang, Jie

PY - 2011/1

Y1 - 2011/1

N2 - 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 the derivatives' ADMErelevant descriptors. The results suggested that these novel compounds had a potential interest for the development of novel and potent vasorelaxant agents.

AB - 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 the derivatives' ADMErelevant descriptors. The results suggested that these novel compounds had a potential interest for the development of novel and potent vasorelaxant agents.

KW - Hypertension

KW - Imperatorin derivatives

KW - Vasodilatory activity

KW - Vasorelaxant agents

UR - https://www.scopus.com/pages/publications/78751534315

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AN - SCOPUS:78751534315

SN - 1573-4064

VL - 7

SP - 18

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JO - Medicinal Chemistry

JF - Medicinal Chemistry

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Design, Synthesis and Preliminary Evaluation of Novel Imperatorin Derivatives as Vasorelaxant Agents

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