Abstract
A series of novel Ligustrazinyl acylguanidines was designed, synthesized and evaluated for their protective effect on injured vascular endothelial cell (ECV-304). The preliminary results demonstrated that some compounds possessed more potent activities than that of Ligustrazine in stimulating replication of the injured endothelial cell. Among the active compounds, compounds 8b, 8f and 8l displayed remarkable antioxidative activity with low EC(50) values of 0.097, 0.059 and 0.094 mM, respectively. Structure-activity relationships were briefly discussed.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antioxidants / chemical synthesis*
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Antioxidants / pharmacology
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Cardiovascular Agents / chemical synthesis*
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Cardiovascular Agents / pharmacology
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Cell Line
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Drug Design
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Endothelial Cells / drug effects
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Endothelial Cells / pathology
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Guanidines / chemical synthesis*
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Guanidines / pharmacology
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Humans
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Inhibitory Concentration 50
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Pyrazines / chemical synthesis*
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Pyrazines / pharmacology
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Structure-Activity Relationship
Substances
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Antioxidants
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Cardiovascular Agents
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Guanidines
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Pyrazines
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tetramethylpyrazine