The alkaloid piperine has always attracted the interest of pharmaceutical
botanists for its biological activities and pharmacokinetics-modulating properties. It is
currently used in combination with other compounds for the treatment of several
diseases. Starting from its peculiar structure, medicinal chemists have explored the
chemical space around the amide portion, the conjugated double bond chain and the
benzodioxole ring. This approach led to a large plethora of derivatives, which
diversified the properties of the parent compound or improved its potency against
specific targets or biological systems. In this chapter, several classes of piperine
derivatives have been discussed and classified according to the proposed therapeutic
use, with a particular attention on their structure-activity relationships and biological
activity values.
Keywords: Acaricidal, Antimicrobial activity, Anti-cancer activity, Anti-protozoal, Insecticidal, MAO-B inhibitor, Natural compounds, Neuroinflammation, Piperine, PPAR, SAR analysis, Vitiligo
