Piperine is the main constituent of pepper, a commonly used kitchen spice and has been reported
to possess various pharmacological activities. The structural features, an aromatic ring with a
methylenedioxy bridge, a conjugated dienone system and a piperidine ring constituting an amide
bond, possessed by the molecule have been considered important for the molecule to exhibit an array
of bioactivities. Several modifications of above structural units have affected the biological properties
of piperine, either enhancing or in some cases completely abolishing the activity. The present review
emphasizes on the synthetic aspects of piperine along with the structure-activity relationships of its derivatives
so as to rationalize the discovery of newer piperine based molecules.
Keywords: Anti-cancer, Anti-leishmanial, Anti-trypanosomal, Piperine, Piper nigrum, Structure-activity relationship.
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