Abstract
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.
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