A Series of Novel Bioactive Cyclic Peptides: Synthesis by Head-to-Tail Cyclization Approach, Antimicrobial Activity and Molecular Docking Studies

摘要

A new series of cyclic antimicrobial peptides (AMPs) containing D/L-α-amino acids have been designed and characterized by spectroscopic techniques. Newly synthesized cyclic peptides were tested for antibacterial and antifungal activities in the hopes of discovering novel clues that may be used to create effective anti-microbial medicine. Those cyclic AMPs demonstrated good antibacterial activity against Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus and that was comparable to reference drug Imipenem, as well as good antifungal activity against microbial strains Aspergillus Flavus, Candida Albicans and Candida GlabarataI that was comparable to reference drug Miconazole. In continuous, molecular docking study of the targeted cyclic peptides revealed that they exhibited promising binding interaction networks with DNA gyrase and lanosterol-14 alpha demethylase, which showed the correlation between biologic activity and docking score of the synthesized analogs.