Abstract
Growing evidence suggests a role for the endocannabinoid (EC) system, in intestinal inflammation and compounds inhibiting anandamide degradation offer a promising therapeutic option for the treatment of inflammatory bowel diseases. In this paper, we report the first series of carboxamides derivatives possessing FAAH inhibitory activities. Among them, compound 39 displayed significant inhibitory FAAH activity (IC(50)=0.088 μM) and reduced colitis induced by intrarectal administration of TNBS.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amidohydrolases / antagonists & inhibitors
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Amidohydrolases / chemistry*
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Amidohydrolases / metabolism
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Animals
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Colitis / prevention & control*
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Disease Models, Animal
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Enzyme Activation / drug effects
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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Humans
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Inhibitory Concentration 50
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Isoxazoles / chemistry*
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Isoxazoles / pharmacology*
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Mice
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Mice, Inbred C57BL
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Models, Molecular
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Molecular Structure
Substances
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Enzyme Inhibitors
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Isoxazoles
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Amidohydrolases
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fatty-acid amide hydrolase