Sirtuin inhibitors (or SIRT inhibitors) are a class of compounds that interfere with the function of sirtuins. SIRT activity is linked to DNA repair, inflammation, neuroprotection, healthy aging, and many other processes. There is a growing interest in the discovery of small molecules altering SIRT activity because their modulation could have beneficial effects on human diseases. SIRT inhibition has been suggested in the treatment of cancer, immunodeficiency virus infections, the prevention or treatment of parasitic diseases, and neurodegenerative diseases.