Author(s): Meghan Duncan, Robert B. Perni, James L. Ellis, George P. Vlasuk, Michael R. Jirousek, Joseph J. Nunes, Jill C. Milne, Peter J. Elliot, Vipin Suri, Akanksha Gupta, Kristina Kriksciukaite, Marie Yeager, Pui Yee Ng, Angela Tornblom, Siva Lavu, Jesse J. Smith, Jeffrey Song, Thomas V. Riera, David P. Carney, Amy V. Lynch, Christopher J. Oalmann, Chi B. Vu, Jeremy S. Disch and Jean E. Bemis
Page: [793 - 797] Pages: 5
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We have identified SRT2104 (4) as the first direct synthetic SIRT1 activator clinical candidate. The compound was derived from the optimization of a previously described imidazo[1,2-b]thiazole scaffold. SRT2104 was selected as a development candidate based on a combination of biochemical activity and pharmacokinetic profile. The in vivo characteristics of SRT2104 were superior to those of analogues with similar activation profiles. The overall preclinical profile suggests that the compound has potential to provide therapeutic benefit in a clinical setting.
Keywords: Activator, Imidazothiazole, SIRT1, Sirtuin, SRT1720, SRT2104.
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