Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors
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.
Xin, Zhili,Zhao, Hongyu,Serby, Michael D.,Liu, Bo,Liu, Mei,Szczepankiewicz, Bruce G.,Nelson, Lissa T.J.,Smith, Harriet T.,Suhar, Tom S.,Janis, Rich S.,Cao, Ning,Camp, Heidi S.,Collins, Christine A.,Sham, Hing L.,Surowy, Teresa K.,Liu, Gang
supporting information; scheme or table
p. 4298 - 4302
(2009/04/06)
Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors
Stearoyl-CoA desaturase 1 (SCD1) catalyzes the committed step in the biosynthesis of monounsaturated fatty acids from saturated, long-chain fatty acids. Studies with SCD1 knockout mice have established that these animals are lean and protected from leptin
Liu, Gang,Lynch, John K.,Freeman, Jennifer,Liu, Bo,Xin, Zhili,Zhao, Hongyu,Serby, Michael D.,Kym, Philip R.,Suhar, Tom S.,Smith, Harriet T.,Cao, Ning,Yang, Ruojing,Janis, Rich S.,Krauser, Joel A.,Cepa, Steven P.,Beno, David W. A.,Sham, Hing L.,Collins, Christine A.,Surowy, Teresa K.,Camp, Heidi S.
p. 3086 - 3100
(2008/02/10)
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