SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Basic Information
ID: ALA1154928
Journal: Bioorg Med Chem Lett
Title: SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Authors: Ramtohul YK, Black C, Chan CC, Crane S, Guay J, Guiral S, Huang Z, Oballa R, Xu LJ, Zhang L, Li CS.
Abstract: Elevated stearoyl-CoA desaturase (SCD) activity has been linked to a number of metabolic disorders including obesity and type II diabetes. Compound 3j, a potent SCD inhibitor (human HepG2 IC(50)=1nM) was identified from the optimization of a lead thiazole compound MF-152 with over 100-fold improvement in potency. In a 4-week chronic oral dosing at 0.2mg/kg, 3j gave a robust 24% prevention of body weight gain in mice fed on a high fat diet accompanied with an improved metabolic profile on insulin and glucose levels.
CiteXplore: 20137926
DOI: 10.1016/j.bmcl.2010.01.083
Patent ID: ┄