138676-18-3Relevant academic research and scientific papers
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.
Inhibitors of Diacylglycerol Acyltransferase
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, (2010/06/22)
Provided herein are amides containing at least a four ring structure, which are inhibitors of diacylglycerol acyltransferase and are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
Diacylglycerol acyltransferase inhibitors
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Page/Page column 22, (2010/11/27)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
Regioselectivity in the Lithiation of Methyl-substituted Thiazole- and Oxazole-Carboxylic Acids and Carboxamides: General Methods for the Elaboration of Trisubstituted Thiazoles and Oxazoles
Cornwall, Philip,Dell, Colin P.,Knight, David W.
, p. 2417 - 2428 (2007/10/02)
A number of anionic intermediates have been developed which are suitable for the elaboration of trisubstituted thiazoles and oxazoles.Thus, deprotonation of 2,4-dimethylthiazole-5-carboxylic acid 9 using either BuLi or LDA occurs regiospecifically at the
