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. 2012 Jan 15;22(2):980-4.
doi: 10.1016/j.bmcl.2011.12.002. Epub 2011 Dec 8.

Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series

Nicolas Lachance  1 , Yves Gareau, Sébastien Guiral, Zheng Huang, Elise Isabel, Jean-Philippe Leclerc, Serge Léger, Evelyn Martins, Christian Nadeau, Renata M Oballa, Stéphane G Ouellet, David A Powell, Yeeman K Ramtohul, Geoffrey K Tranmer, Thao Trinh, Hao Wang, Lei Zhang
Affiliations

Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series

Nicolas Lachance et al. Bioorg Med Chem Lett. .

Abstract

Inhibition of stearoyl-CoA desaturase (SCD) activity represents a potential novel mechanism for the treatment of metabolic disorders including obesity and type II diabetes. To circumvent skin and eye adverse events observed in rodents with systemically-distributed SCD inhibitors, our research efforts have been focused on the search for new and structurally diverse liver-targeted SCD inhibitors. This work has led to the discovery of novel, potent and structurally diverse liver-targeted bispyrrolidine 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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