Synthesis And Biological Evaluation Of 5-(3,4- Methylenedioxyphenyl)-2,4-Pentadienoic Acid Derivatives As Potent Antimicrobial And Cytotoxicity Agents
Journal Title: IOSR Journal of Applied Chemistry (IOSR-JAC) - Year 2018, Vol 11, Issue 5
Abstract
Dark pepper (Piper nigrum L.) has for quite some time been viewed as a spice added to numerous nourishments and it is additionally considered as a medicinal plant. The predominant compound got from ethanolic concentrate of P. nigrum, the piperine, was crystallized. Piperine, a noteworthy alkaloid in dark pepper is a standout amongst the most encouraging bioenhancers till date. Piperic acid was synthesized by alkaline hydrolysis of the cleaned piperine. A progression of piperine analogs were incorporated by the buildup of piperic acid with various substituted aniline (3a-3e). The synthesized compounds (4a– 4e) were assessed for their anticancer activity against human growth cell lines (HEPG 2, Liver Cancer cell line and MCF-7, Breast Cancer cell line) and antibacterial activity against human pathogens (Escherichia coli, Bacillus subtilis, Staphylococcus aureus, Vibrio cholerae and Pseudomonas aeruginosa). The efficacies of the synthesized compounds (4a-4e) were better than those of piperine in all tried human cancer cell lines. Among the derivatives, 4d indicated huge anticancer action against breast cancer cell line(MCF-7) with IC50 of 3.78 µmol and 4b indicated huge action against liver cancer cell line (HEPG 2). The antibacterial activity of the derivates was additionally observed to be better for compound 4b and 4d than that of other derivatives. Therefore the approach is novel as the richly accessible common item piperine is used as precursor for the synthesis of new potential antimicrobial and anticancer agents.
Authors and Affiliations
A. Ramesh, P. Sundarraj, Dr. J. Balamani
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