1246749-62-1Relevant articles and documents
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series
Lachance, Nicolas,Gareau, Yves,Guiral, Sebastien,Huang, Zheng,Isabel, Elise,Leclerc, Jean-Philippe,Leger, Serge,Martins, Evelyn,Nadeau, Christian,Oballa, Renata M.,Ouellet, Stephane G.,Powell, David A.,Ramtohul, Yeeman K.,Tranmer, Geoffrey K.,Trinh, Thao,Wang, Hao,Zhang, Lei
scheme or table, p. 980 - 984 (2012/03/26)
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.