Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities |
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Authors: | Haifeng Tang Yan Yan Zhe Feng Reynalda K. de Jesus Lihu Yang Dorothy A. Levorse Karen A. Owens Taro E. Akiyama Raynald Bergeron Gino A. Castriota Thomas W. Doebber Kenneth P. Ellsworth Michael E. Lassman Cai Li Margaret S. Wu Bei B. Zhang Kevin T. Chapman Sander G. Mills Joel P. Berger Alexander Pasternak |
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Affiliation: | Department of Medicinal Chemistry, Metabolic Disorders, Drug Metabolism and Pharmacology, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA |
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Abstract: | A new series of thiazole-substituted 1,1,1,3,3,3-hexafluoro-2-propanols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Key analogs caused dose-dependent decreases in food intake and body weight in obese mice. Acute treatment with these compounds also led to a drop in elevated blood glucose in a murine model of type II diabetes. |
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