Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Bioorganic & Medicinal Chemistry Letters(2019)
摘要
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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关键词
Parallel medicinal chemistry,High throughput purification,DGAT1 inhibitor,Triglyceride,Benzimidazole,ACAT1,A2A receptor,Cyclohexane acetic acid,Lipid tolerance test,Pharmacokinetics
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