2. Academic Validation
  3. Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438)

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

Affiliation

  • 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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