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  • Title: Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
    Author: Léger S, Black WC, Deschenes D, Dolman S, Falgueyret JP, Gagnon M, Guiral S, Huang Z, Guay J, Leblanc Y, Li CS, Massé F, Oballa R, Zhang L.
    Journal: Bioorg Med Chem Lett; 2010 Jan 15; 20(2):499-502. PubMed ID: 20004097.
    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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