The discovery of potent benzimidazole stearoyl-CoA desaturase (SCD1) inhibitors by ligand-based virtual screening is described. ROCS 3D-searching gave a favorable chemical motif that was subsequently optimized to arrive at a chemical series of potent and promising SCD1 inhibitors. In particular, compound SAR224 was selected for further pharmacological profi領(lǐng) based on favorable in vitro data. After oral administration to male ZDF rats, this compound significantly decreased the serum fatty acid desaturation index, thus providing conclusive evidence for SCD1 inhibition in vivo by SAR224. Biotage 微波合成儀 Initiator+ Biotage 微波合成儀 Initiator Biotage 微波合成儀 Initiator+ Robot 8 Biotage 微波合成儀 Initiator+ Robot 60