Bioorganic & Medicinal Chemistry Letters 2008-08-01

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

Zhili Xin, Hongyu Zhao, Michael D Serby, Bo Liu, Mei Liu, Bruce G Szczepankiewicz, Lissa T J Nelson, Harriet T Smith, Tom S Suhar, Rich S Janis, Ning Cao, Heidi S Camp, Christine A Collins, Hing L Sham, Teresa K Surowy, Gang Liu, Zhili Xin, Hongyu Zhao, Michael D. Serby, Bo Liu, Mei Liu, Bruce G. Szczepankiewicz, Lissa T.J. Nelson, Harriet T. Smith, Tom S. Suhar, Rich S. Janis, Ning Cao, Heidi S. Camp, Christine A. Collins, Hing L. Sham, Teresa K. Surowy, Gang Liu

文献索引：Bioorg. Med. Chem. Lett. 18(15) , 4298-302, (2008)

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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 lowering effects.