Abstract
A series of novel Ligustrazinyl amides was designed, synthesized and evaluated for their protective effect on the injured vascular endothelial cells. The preliminary results demonstrated that some compounds possessed more potent activities than that of Ligustrazine in stimulating replication of the injured human umbilical vascular endothelial cells (HUVECs) that is damaged by hydrogen peroxide. Among the active compounds, compounds 8i, 8t and 8u exhibited the highest potency with low EC50 values of 0.037, 0.070 and 0.055 mM, respectively. Structure-activity relationships were briefly discussed.
Keywords: Ligustrazine, pyrazine amides, synthesis, cardiovascular disease.
Medicinal Chemistry
Title:Ligustrazine Derivatives. Part 8: Design, Synthesis, and Preliminary Biological Evaluation of Novel Ligustrazinyl Amides as Cardiovascular Agents
Volume: 10 Issue: 1
Author(s): Zhenyu Li, Fang Yu, Lei Cui, Wenmin Chen, Shouxun Wang, Peng Zhan, Yuemao Shen and Xinyong Liu
Affiliation:
Keywords: Ligustrazine, pyrazine amides, synthesis, cardiovascular disease.
Abstract: A series of novel Ligustrazinyl amides was designed, synthesized and evaluated for their protective effect on the injured vascular endothelial cells. The preliminary results demonstrated that some compounds possessed more potent activities than that of Ligustrazine in stimulating replication of the injured human umbilical vascular endothelial cells (HUVECs) that is damaged by hydrogen peroxide. Among the active compounds, compounds 8i, 8t and 8u exhibited the highest potency with low EC50 values of 0.037, 0.070 and 0.055 mM, respectively. Structure-activity relationships were briefly discussed.
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Cite this article as:
Li Zhenyu, Yu Fang, Cui Lei, Chen Wenmin, Wang Shouxun, Zhan Peng, Shen Yuemao and Liu Xinyong, Ligustrazine Derivatives. Part 8: Design, Synthesis, and Preliminary Biological Evaluation of Novel Ligustrazinyl Amides as Cardiovascular Agents, Medicinal Chemistry 2014; 10 (1) . https://dx.doi.org/10.2174/157340641130900042
DOI https://dx.doi.org/10.2174/157340641130900042 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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