Bioorganic and Medicinal Chemistry Letters p. 1380 - 1385 (2019)
Update date:2022-08-03
Topics:
Yu, Yang
Wu, Zhicai
Shi, Zhi-Cai
He, Shuwen
Lai, Zhong
Cernak, Timothy A.
Vachal, Petr
Liu, Min
Liu, Jian
Hong, Qingmei
Jian, Tianying
Guiadeen, Deodial
Krikorian, Arto
Sperbeck, Donald M.
Verras, Andreas
Sonatore, Lisa M.
Murphy, Beth A.
Wiltsie, Judyann
Chung, Christine C.
Gorski, Judith N.
Liu, Jinqi
Xiao, Jianying
Wolff, Michael
Tong, Sharon X.
Madeira, Maria
Karanam, Bindhu V.
Shen, Dong-Ming
Balkovec, James M.
De Vita, Robert J.
Pinto, Shirly
Nargund, Ravi P.
The parallel medicinal chemistry (PMC) was effectively applied to accelerate the optimization of diacylglycerol O-acyltransferase I (DGAT-1) inhibitors. Through a highly collaborative and iterative library design, synthesis and testing, a benzimidazole lead was rapidly and systematically advanced to a highly potent, selective and bioavailable DGAT1 inhibitor with the potential for further development.
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