Abstract
We investigated N-adamantyl-N'-phenyl urea derivatives as simple sEH inhibitors. Salicylate ester derivatives have high inhibitory activities against human sEH, while the free benzoic acids are less active. The methyl salicylate derivative is a potent sEH inhibitor, which also has high metabolic and chemical stabilities; suggesting that such inhibitors are potential lead molecule for bioactive compounds acting in vivo.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology
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Benzoates / chemistry
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Chemistry, Pharmaceutical / methods
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Drug Design
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Epoxide Hydrolases / antagonists & inhibitors*
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Epoxide Hydrolases / chemistry
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Humans
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Hydrogen Bonding
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Hydrolysis
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Hypertension / drug therapy
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Inhibitory Concentration 50
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Kinetics
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Models, Chemical
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Salicylates / chemistry*
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Spectrometry, Fluorescence / methods
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Urea / chemistry*
Substances
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Anti-Inflammatory Agents
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Benzoates
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Salicylates
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Urea
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Epoxide Hydrolases