Capsaicin derivatives: Synthesis and biological activity

Abstract Capsaicin is the main active ingredient of chili peppers and the most pungent alkaloid. It is reported that capsaicin has many pharmacological effects such as analgesia, anticancer, anti‐inflammatory, antibacterial, and anti‐obesity. However, the application of capsaicin is limited by its adverse side effects, such as stomach irritation, stomach cramps, and burning sensation. In recent years, many capsaicin derivatives have been synthesized and their biological activities have been evaluated. Some capsaicin derivatives have shown promising activities in cells and animal models. Herein, we described the synthesis and biological activity of capsaicin and its derivatives. It is hoped that the insights obtained in this perspective will facilitate the synthesis of a second generation of capsaicin analogs with improved biological activities.