916889-48-0Relevant academic research and scientific papers
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors
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)
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.
CYCLIC AMINE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
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, (2008/06/13)
Cyclic amine derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and
Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors
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)
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
AZACYCLOHEXANE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
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Page/Page column 37, (2008/06/13)
Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
