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Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins

Title
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins
Authors
Kamisuki S.Shirakawa T.Kugimiya A.Abu-Elheiga L.Park Choo H.-Y.Yamada K.Shimogawa H.Wakil S.J.Uesugi M.
Ewha Authors
박혜영
SCOPUS Author ID
박혜영scopus
Issue Date
2011
Journal Title
Journal of Medicinal Chemistry
ISSN
0022-2623JCR Link
Citation
vol. 54, no. 13, pp. 4923 - 4927
Indexed
SCI; SCIE; SCOPUS scopus
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. © 2011 American Chemical Society.
DOI
10.1021/jm200304y
Appears in Collections:
약학대학 > 약학과 > Journal papers
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