Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the …

…, SJ Wertheimer, M Ahmad, AWH Cheung…

文献索引：Qian, Yimin; Wertheimer, Stanley J.; Ahmad, Mushtaq; Cheung, Adrian Wai-Hing; Firooznia, Fariborz; Hamilton, Matthew M.; Hayden, Stuart; Li, Shiming; Marcopulos, Nicholas; McDermott, Lee; Tan, Jenny; Yun, Weiya; Guo, Liang; Pamidimukkala, Anjula; Chen, Yingsi; Huang, Kuo-Sen; Ramsey, Gwendolyn B.; Whittard, Toni; Conde-Knape, Karin; Taub, Rebecca; Rondinone, Cristina M.; Tilley, Jefferson; Bolin, David Journal of Medicinal Chemistry, 2011 , vol. 54, # 7 p. 2433 - 2446

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被引用次数: 27

摘要

Diacylglycerol acyltransferase-1 (DGAT-1) is the enzyme that catalyzes the final and committed step of triglyceride formation, namely, the acylation of diacylglycerol with acyl coenzyme A. DGAT-1 deficient mice demonstrate resistance to weight gain on high fat diet, improved insulin sensitivity, and reduced liver triglyceride content. Inhibition of DGAT-1 thus represents a potential novel approach for the treatment of obesity, dyslipidemia, and ...