Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors

…, B Liu, M Liu, BG Szczepankiewicz, LTJ Nelson…

文献索引：Xin, Zhili; Zhao, Hongyu; Serby, Michael D.; Liu, Bo; Liu, Mei; Szczepankiewicz, Bruce G.; Nelson, Lissa T.J.; Smith, Harriet T.; Suhar, Tom S.; Janis, Rich S.; Cao, Ning; Camp, Heidi S.; Collins, Christine A.; Sham, Hing L.; Surowy, Teresa K.; Liu, Gang Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 15 p. 4298 - 4302

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被引用次数: 46

摘要

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 ...