Discovery of dimethyl pent-4-ynoic acid derivatives, as potent and orally bioavailable DGAT1 inhibitors that suppress body weight in diet-induced mouse obesity model.

[1]  T. Gilmore,et al.  Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans. , 2017, Journal of medicinal chemistry.

[2]  Shirly Pinto,et al.  Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors. , 2013, Journal of medicinal chemistry.

[3]  B. Hubbard,et al.  The DGAT1 inhibitor Pradigastat Decreases Chylomicron Secretion and Prevents Postprandial Triglyceride Elevation in Humans , 2013 .

[4]  Magnus J. Johansson,et al.  Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687). , 2012, Journal of medicinal chemistry.

[5]  D. Gaudet,et al.  The DGAT1 Inhibitor LCQ908 Decreases Triglyceride Levels in Patients with the Familial Chylomicronemia Syndrome , 2012 .

[6]  M. Munchhof,et al.  Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3-d]pyrimidine core. , 2011, Bioorganic & medicinal chemistry letters.

[7]  Eliot Sugarman,et al.  Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1. , 2011, ACS medicinal chemistry letters.

[8]  M. Connelly,et al.  High-content assays for evaluating cellular and hepatic diacylglycerol acyltransferase activity , 2010, Journal of Lipid Research.

[9]  A. Souers,et al.  In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia. , 2010, European journal of pharmacology.

[10]  A. Turnbull,et al.  Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. , 2009, Journal of medicinal chemistry.

[11]  A. Souers,et al.  Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. , 2008, Journal of medicinal chemistry.

[12]  Robert V Farese,et al.  Lipopenia and Skin Barrier Abnormalities in DGAT2-deficient Mice* , 2004, Journal of Biological Chemistry.

[13]  H. C. Chen,et al.  DGAT and triglyceride synthesis: a new target for obesity treatment? , 2000, Trends in cardiovascular medicine.

[14]  Joseph A. Miller,et al.  Synthesis of 2,6-bis(trifluoromethyl)phenol and its elaboration into metabolism-resistant analogs of tebufelone , 1993 .