化药新药研发其他>方法开发检测 | 通过Biotage Initiator微波合成进行苯并咪唑类化合物的微波合成耐士科技-上海鑫欣生物科技有限公司

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应用领域	制药/生物制药
检测样本	化药新药研发
检测项目	其他>方法开发
参考标准	GB/T 8****

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 profiling 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.

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