Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: from systemic to liver-targeting inhibitors.
Basic Information
ID: ALA1833926
Journal: Bioorg Med Chem Lett
Title: Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: from systemic to liver-targeting inhibitors.
Authors: Ramtohul YK, Powell D, Leclerc JP, Leger S, Oballa R, Black C, Isabel E, Li CS, Crane S, Robichaud J, Guay J, Guiral S, Zhang L, Huang Z.
Abstract: Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for efficacy and to avoid SCD1 inhibition in the skin and eyes where adverse effects were previously observed in rodents, representative systemically-distributed SCD1 inhibitors were converted into liver-targeting SCD1 inhibitors.
CiteXplore: 21871798
DOI: 10.1016/j.bmcl.2011.08.037
Patent ID: ┄