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Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities

✍ Scribed by 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


Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
363 KB
Volume
20
Category
Article
ISSN
0960-894X

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✦ Synopsis


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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