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Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series. 2012
Nicolas Lachance, and
Sébastien Guiral, and
Zheng Huang, and
Jean-Philippe Leclerc, and
Chun Sing Li, and
Renata M Oballa, and
Yeeman K Ramtohul, and
Hao Wang, and
Jin Wu, and
Lei Zhang
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, 16711 TransCanada Hwy, Kirkland, Quebec, Canada H9H 3L1. nicolas.lachance21@gmail.com
Elevated levels of stearoyl-CoA desaturase (SCD) activity have been implicated in metabolic disorders such as obesity and type II diabetes. To circumvent skin and eye adverse events observed in rodents with systemically-distributed inhibitors, our research efforts have been focused on the search for new liver-targeting compounds. This work has led to the discovery of novel, potent and liver-selective acyclic linker SCD inhibitors. These compounds possess suitable cellular activity and pharmacokinetic properties to inhibit liver SCD activity in a mouse pharmacodynamic model.
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Journal of medicinal chemistry,
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Bioorganic & medicinal chemistry letters,
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Progress in lipid research,
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Yeeman K Ramtohul, and
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Biochemical genetics,
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Nature chemical biology,
