Abstract
A series of thiadiazolopiperazinyl aryl urea fatty acid amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties are presented.
MeSH terms
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Amidohydrolases / antagonists & inhibitors*
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Amidohydrolases / deficiency
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Amidohydrolases / genetics
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Animals
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Mice
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Mice, Knockout
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Piperazines / chemistry
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Piperazines / pharmacokinetics
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Piperazines / pharmacology*
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Thiadiazoles / chemistry
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Thiadiazoles / pharmacokinetics
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Thiadiazoles / pharmacology*
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Urea / analogs & derivatives*
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Urea / chemistry
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Urea / pharmacokinetics
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Urea / pharmacology*
Substances
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Piperazines
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Thiadiazoles
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Urea
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Amidohydrolases
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fatty-acid amide hydrolase