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  • Title: Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.
    Author: Vu CB, Bemis JE, Disch JS, Ng PY, Nunes JJ, Milne JC, Carney DP, Lynch AV, Smith JJ, Lavu S, Lambert PD, Gagne DJ, Jirousek MR, Schenk S, Olefsky JM, Perni RB.
    Journal: J Med Chem; 2009 Mar 12; 52(5):1275-83. PubMed ID: 19199480.
    Abstract:
    A series of imidazo[1,2-b]thiazole derivatives is shown to activate the NAD(+)-dependent deacetylase SIRT1, a potential new therapeutic target to treat various metabolic disorders. This series of compounds was derived from a high throughput screening hit bearing an oxazolopyridine core. Water-solubilizing groups could be installed conveniently at either the C-2 or C-3 position of the imidazo[1,2-b]thiazole ring. The SIRT1 enzyme activity could be adjusted by modifying the amide portion of these imidazo[1,2-b]thiazole derivatives. The most potent analogue within this series, namely, compound 29, has demonstrated oral antidiabetic activity in the ob/ob mouse model, the diet-induced obesity (DIO) mouse model, and the Zucker fa/fa rat model.
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