- Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Bioorganic & medicinal chemistry letters (2008-07-18)
Zhili Xin, Hongyu Zhao, Michael D Serby, Bo Liu, Mei Liu, Bruce G Szczepankiewicz, Lissa T J Nelson, Harriet T Smith, Tom S Suhar, Rich S Janis, Ning Cao, Heidi S Camp, Christine A Collins, Hing L Sham, Teresa K Surowy, Gang Liu
PMID18632269
ZUSAMMENFASSUNG
A series of structurally novel stearoyl-CoA desaturase1 (SCD1) inhibitors has been identified via molecular scaffold manipulation. Preliminary structure-activity relationship (SAR) studies led to the discovery of potent, and orally bioavailable piperidine-aryl urea-based SCD1 inhibitors. 4-(2-Chlorophenoxy)-N-[3-(methyl carbamoyl)phenyl]piperidine-1-carboxamide 4c exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.
MATERIALIEN