Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC)
Yang Yu1, Zhicai Wu1, Zhi-Cai Shi1
1Discovery and Preclinical Sciences, Merck & Co. Inc, 2000 Galloping Hill Road, Kenilworth, NJ 07033, United States.
Bioorganic & Medicinal Chemistry Letters
|April 7, 2019
Abstract:
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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