460081-28-1Relevant articles and documents
Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors
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
, p. 7205 - 7209 (2012/01/15)
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 25 also demonstrated in vivo efficacy in a diet-induced obesity (DIO) rat model.
Ethyl 2-chlorooxazole-4-carboxylate: A versatile intermediate for the synthesis of substituted oxazoles
Hodgetts, Kevin J.,Kershaw, Mark T.
, p. 2905 - 2907 (2007/10/03)
(formula presented) R1 = Ar, Het, alkenyl R2 = H, Ar, Het, alkenyl, alkynyl R3 = H, CO2H, Ar, Het, alkenyl, alkynyl By using a sequence of regiocontrolled halogenation and palladium-catalyzed coupling reactions,