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Bioorg Med Chem Lett. 2013 Dec 15;23(24):6773-6. doi: 10.1016/j.bmcl.2013.09.096. Epub 2013 Oct 9.

4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs.

Author information

  • 1Cardiovascular and Metabolism Research, Janssen Research and Development, LLC, Welsh & McKean Roads, Spring House, PA 19477, USA. Electronic address: shyhyang99@yahoo.com.

Abstract

A new series of urea-based, 4-bicyclic heteroaryl-piperidine derivatives as potent SCD1 inhibitors is described. The structure-activity relationships focused on bicyclic heteroarenes and aminothiazole-urea portions are discussed. A trend of dose-dependent decrease in body weight gain in diet-induced obese (DIO) mice is also demonstrated.

KEYWORDS:

Desaturation index; Obesity; SCD1 inhibitors; Stearoyl-CoA desaturase

PMID:
24153205
DOI:
10.1016/j.bmcl.2013.09.096
[PubMed - indexed for MEDLINE]
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