Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors

G Liu, JK Lynch, J Freeman, B Liu, Z Xin…

文献索引：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. Journal of Medicinal Chemistry, 2007 , vol. 50, # 13 p. 3086 - 3100

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被引用次数: 80

摘要

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 deficiency-induced and diet-induced obesity, with greater whole body insulin sensitivity than wild-type animals. In this work, we have discovered a series of potent, selective, orally ...