Abstract
A series of novel Ligustrazine derivatives was designed, synthesized, and assayed for their protective effects on damaged ECV-304 cells and antiplatelet aggregation activities. The results showed that most Ligustrazine derivatives exhibited lower EC(50) values for protective effects on the ECV-304 cells damaged by hydrogen peroxide in comparison with Ligustrazine. And some Ligustrazine derivatives presented better antiplatelet aggregation activities than Ligustrazine. The derivatives containing the bisphenylmethyl pharmacophore (7a-c) exhibited highest potency. Compound 7a displayed most potential protective effects on the ECV-304 cells damaged by hydrogen peroxide, and compound 7c was found to be the most active antiplatelet aggregation agent. 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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Animals
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Blood Platelets / drug effects
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Cell Line
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Chromatography, Thin Layer
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Drug Design
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Endothelial Cells / drug effects*
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Humans
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Hydrogen Peroxide / antagonists & inhibitors
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Hydrogen Peroxide / toxicity
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In Vitro Techniques
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Oxidants / antagonists & inhibitors
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Oxidants / toxicity
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Platelet Aggregation Inhibitors / chemical synthesis*
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Platelet Aggregation Inhibitors / pharmacology*
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Pyrazines / chemical synthesis*
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Pyrazines / pharmacology*
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Rabbits
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Spectrometry, Mass, Electrospray Ionization
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Spectrophotometry, Infrared
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Spectroscopy, Fourier Transform Infrared
Substances
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Indicators and Reagents
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Oxidants
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Platelet Aggregation Inhibitors
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Pyrazines
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Hydrogen Peroxide
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tetramethylpyrazine