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. 2009 Mar 12;52(5):1275-83.
doi: 10.1021/jm8012954.

Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators

Chi B Vu  1 , Jean E Bemis, Jeremy S Disch, Pui Yee Ng, Joseph J Nunes, Jill C Milne, David P Carney, Amy V Lynch, Jesse J Smith, Siva Lavu, Philip D Lambert, David J Gagne, Michael R Jirousek, Simon Schenk, Jerrold M Olefsky, Robert B Perni
Affiliations

Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators

Chi B Vu et al. J Med Chem. .

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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