Details

Autor(en) / Beteiligte

• 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.

Titel

Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC)

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2019-06, Vol.29 (11), p.1380-1385

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2019

Link zum Volltext

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• [Display omitted] 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.