Abstract
A series of novel 2-azetidinones (beta-lactams) bearing short alkenyl chains at C3 and N1 have been prepared and evaluated in vitro as inhibitors of human FAAH. Compound 9c (1-(4'-pentenoyl-3-(4'-pentenyl)-2-azetidinone)) featured an IC(50) value of 4.5 microM and a good selectivity for FAAH versus MGL.
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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Animals
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Azetidines / pharmacology*
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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 / chemistry
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Escherichia coli / metabolism
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Humans
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Inhibitory Concentration 50
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Magnetic Resonance Spectroscopy
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Models, Chemical
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Pancreatic Elastase / antagonists & inhibitors
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Swine
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beta-Lactams / chemistry
Substances
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2-azetidinone
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Azetidines
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Enzyme Inhibitors
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beta-Lactams
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Pancreatic Elastase
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Amidohydrolases
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fatty-acid amide hydrolase