Piperine and Derivatives: Trends in Structure-Activity Relationships
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Updated: Apr 14, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Inder Pal Singh1, Alka Choudhary
1Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, SAS Nagar, Punjab-160062, India. ipsingh67@yahoo.com.
Abstract:
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.
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