Synthesis and Evaluation of Diarylthiazole Derivatives That Inhibit Activation of Sterol Regulatory Element-Binding Proteins
Journal of Medicinal Chemistry2011Vol. 54(13), pp. 4923–4927
Citations Over TimeTop 11% of 2011 papers
Shinji Kamisuki, Takashi Shirakawa, Akira Kugimiya, Lutfi Abu-Elheiga, Hea‐Young Park Choo, Kohei Yamada, Hiroki Shimogawa, Salih J. Wakil, Motonari Uesugi
Abstract
Fatostatin, a recently discovered small molecule that inhibits activation of sterol regulatory element-binding protein (SREBP), blocks biosynthesis and accumulation of fat in obese mice. We synthesized and evaluated a series of fatostatin derivatives. Our structure-activity relationships led to the identification of N-(4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide (24, FGH10019) as the most potent druglike molecule among the analogues tested. Compound 24 has high aqueous solubility and membrane permeability and may serve as a seed molecule for further development.
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