Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety

[Image: see text] We report the discovery of a novel series of DGAT1 inhibitors in the benzimidazole class with a piperdinyl-oxy-cyclohexanecarboxylic acid moiety. This novel series possesses significantly improved selectivity against the A(2A) receptor, no ACAT1 off-target activity at 10 μM, and hi...

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Main Authors: He, Shuwen, Hong, Qingmei, Lai, Zhong, Yang, David X., Ting, Pauline C., Kuethe, Jeffrey T., Cernak, Timothy A., Dykstra, Kevin D., Sperbeck, Donald M., Wu, Zhicai, Yu, Yang, Yang, Ginger X., Jian, Tianying, Liu, Jian, Guiadeen, Deodial, Krikorian, Arto D., Sonatore, Lisa M., Wiltsie, Judyann, Liu, Jinqi, Gorski, Judith N., Chung, Christine C., Gibson, Jack T., Lisnock, JeanMarie, Xiao, Jianying, Wolff, Michael, Tong, Sharon X., Madeira, Maria, Karanam, Bindhu V., Shen, Dong-Ming, Balkovec, James M., Pinto, Shirly, Nargund, Ravi P., DeVita, Robert J.
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2014
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4207266/
https://ncbi.nlm.nih.gov/pubmed/25349648
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml5003426
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