2. Academic Validation
  3. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors

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

  • Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302. doi: 10.1016/j.bmcl.2008.06.088.
Zhili Xin 1,  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
Affiliations

Affiliation

  • 1 Abbott Laboratories, Global Pharmaceutical Research and Development, 100 Abbott Road, Abbott Park, IL 60064, USA. [email protected]
PMID: 18632269 DOI: 10.1016/j.bmcl.2008.06.088
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.

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