Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors

…, M Ahmad, Y Chen, P Gillespie, K Conde-Knape…

文献索引：Yun, Weiya; Ahmad, Mushtaq; Chen, Yingsi; Gillespie, Paul; Conde-Knape, Karin; Kazmer, Sonja; Li, Shiming; Qian, Yimin; Taub, Rebecca; Wertheimer, Stanley J.; Whittard, Toni; Bolin, David Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 23 p. 7205 - 7209

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被引用次数: 8

摘要

In a discovery effort to find safe and effective DGAT-1 inhibitors, we have identified 2- phenyloxazole 4-carboxamide 1 as a conformationally constrained analog of a hydrazide hit, which was previously identified from high-throughput screening. Further optimization of this series has led to chemically more stable 2-phenyloxazole-based DGAT-1 inhibitor 25 with improved solubility, cell-based activity, and pharmacokinetic properties. Compound ...