Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities
β 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
No coin nor oath required. For personal study only.
β¦ 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.
π SIMILAR VOLUMES
Several compounds, structurally related to the insect-growth regulator Fenvxycarb (l), were designed and synthesized. These compounds were tested as growth inhibitors of Trypanmvma cruzi cells (epimastigotes). Compounds 6,16, 18, and 22 were very active against 7'. cruzi making them promising good c