Abstract
A series of structurally novel stearoyl-CoA desaturase1 (SCD1) inhibitors has been identified via molecular scaffold manipulation. Preliminary structure-activity relationship (SAR) studies led to the discovery of potent, and orally bioavailable piperidine-aryl urea-based SCD1 inhibitors. 4-(2-Chlorophenoxy)-N-[3-(methyl carbamoyl)phenyl]piperidine-1-carboxamide 4c exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.
MeSH terms
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Molecular Structure
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Piperidines / chemical synthesis
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Piperidines / chemistry
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Piperidines / pharmacology*
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Stearoyl-CoA Desaturase / antagonists & inhibitors*
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Structure-Activity Relationship
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Substrate Specificity
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Urea / analogs & derivatives*
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Urea / chemical synthesis*
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Urea / chemistry
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Urea / pharmacology*
Substances
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4-(2-chlorophenoxy)-N-(3-(methyl carbamoyl)phenyl)piperidine-1-carboxamide
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Enzyme Inhibitors
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Piperidines
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Urea
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Stearoyl-CoA Desaturase