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The discovery of potent, selective, orally bioavailable SCD1 inhibitors is reported.
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.