Abstract
Inhibition of soluble epoxide hydrolase (sEH) has been proposed as a new pharmaceutical approach for treating hypertension and vascular inflammation. The most potent sEH inhibitors reported in literature to date are urea derivatives. However, these compounds have limited pharmacokinetic profiles. We investigated non-urea amide derivatives as sEH inhibitors and identified a potent human sEH inhibitor 14-34 having potency comparable to urea-based inhibitors.
Published by Elsevier Ltd.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Amides / chemistry
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology*
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Epoxide Hydrolases / antagonists & inhibitors*
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Fluorescent Dyes / pharmacology
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Humans
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Hydrogen Bonding
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Hypertension / drug therapy
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Inflammation / drug therapy
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Inhibitory Concentration 50
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Microscopy, Fluorescence / methods
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Models, Chemical
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Solubility
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Structure-Activity Relationship
Substances
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Amides
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Enzyme Inhibitors
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Fluorescent Dyes
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Epoxide Hydrolases