Design and synthesis of amide derivatives inspired by capsaicin as potential antibacterial and antitumor agents.

Abstract

Nine amide derivatives inspired by capsaicin (ADICs) were synthesised and evaluated for antibacterial and antitumor activities by a series of standard methods in this study. The results showed that ADICs had good antibacterial and antitumor activity. In the antibacterial assay, their inhibitory rates were over 76.70% at 20 μg/mL, the MIC values were not more than 32 μg/mL, and they exhibited healthy characteristics with MBC values exceeding 128 μg/mL. In antitumor assay, the inhibition rates of the products a3, b3, and c3 with chloroacetamide exceeded 55.00% at 10 μM, and their IC₅₀ values were all less than 8.61 μM; furthermore, injection of products a3 and b3 suppressed the growth of A549 and HCT116 tumour cells transplanted subcutaneously into nude mice. As benign and healthy antibacterial and antitumor agents, the research and development of ADICs are of important realistic significance to their application in the food and pharmaceutical industries.