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Sirtuin 1-Activating Compounds: Discovery of a Class of Thiazole-Based Derivatives.


ABSTRACT: Sirtuin 1 (SIRT1) is a NAD+-dependent deacetylase implicated in various biological and pathological processes, including cancer, diabetes, and cardiovascular diseases. In recent years, SIRT1-activating compounds have been demonstrated to exert cardioprotective effects. Therefore, this enzyme has become a feasible target to treat cardiovascular diseases, and many SIRT1 activators, of a natural or synthetic origin, have been identified. In the present work, we developed thiazole-based SIRT1 activators, which showed remarkably higher SIRT1 activation potencies compared with those of the reference compound resveratrol when tested in enzymatic assays. Thiazole 8, a representative compound of this series, was also subjected to further pharmacological investigations, where it wa

SUBMITTER: Bononi G 

PROVIDER: S-EPMC9570679 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature