4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: Urea-based analogs

…, Y Liang, JM Lenhard, KT Demarest, WV Murray

Index: Yang, Shyh-Ming; Tang, Yuting; Zhang, Rui; Lu, Huajun; Kuo, Gee-Hong; Gaul, Michael D.; Li, Yaxin; Ho, George; Conway, James G.; Liang, Yin; Lenhard, James M.; Demarest, Keith T.; Murray, William V. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6773 - 6776

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Citation Number: 4

Abstract

Abstract A new series of urea-based, 4-bicyclic heteroaryl-piperidine derivatives as potent SCD1 inhibitors is described. The structure–activity relationships focused on bicyclic heteroarenes and aminothiazole–urea portions are discussed. A trend of dose-dependent decrease in body weight gain in diet-induced obese (DIO) mice is also demonstrated.

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