Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438)

  • Bioorg Med Chem Lett. 2010 Jan 15;20(2):499-502. doi: 10.1016/j.bmcl.2009.11.111.
Serge Léger  1 ,  W Cameron Black ,  Denis Deschenes ,  Sarah Dolman ,  Jean-Pierre Falgueyret ,  Marc Gagnon ,  Sébastien Guiral ,  Zheng Huang ,  Jocelyne Guay ,  Yves Leblanc ,  Chun-Sing Li ,  Frédéric Massé ,  Renata Oballa ,  Lei Zhang
Affiliations
  • 1. Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe-Claire-Dorval, Québec, Canada H9R 4P8.
PMID: 20004097 DOI: 10.1016/j.bmcl.2009.11.111
Abstract

A series of stearoyl-CoA desaturase 1 (SCD1) inhibitors were developed. Investigations of enzyme potency and metabolism led to the identification of the thiadiazole-pyridazine derivative MF-438 as a potent SCD1 inhibitor. MF-438 exhibits good pharmacokinetics and metabolic stability, thereby serving as a valuable tool for further understanding the role of SCD inhibition in biological and pharmacological models of diseases related to metabolic disorders.

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