Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
Basic Information
ID: ALA1949632
Journal: Bioorg Med Chem Lett
Title: Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
Authors: Lachance N, Guiral S, Huang Z, Leclerc JP, Li CS, Oballa RM, Ramtohul YK, Wang H, Wu J, Zhang L.
Abstract: 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.
CiteXplore: 22101133
DOI: 10.1016/j.bmcl.2011.10.070
Patent ID: ┄