| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376383 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
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.
Graphical abstractThe discovery of potent, selective, orally bioavailable SCD1 inhibitors is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,