abstract |
The invention relates to a cyclic peptide with antibacterial activity and a synthesis method thereof, belonging to the technical field of biopharmaceuticals. The main technical scheme is that the present invention uses m-dibromobenzyl as a small molecule auxiliary reagent under room temperature and slightly alkaline environment, and utilizes the sulfhydryl groups of the two cysteines in the linear peptide to undergo a nucleophilic substitution reaction with it, so that the linear Peptide cyclization. This linear peptide cyclization method has mild reaction conditions and is extremely easy to implement. The reaction speed is fast, the time is short, and it can be completed within 2 hours. The cyclization efficiency can reach more than 90%, the total yield of the cyclic peptide can reach more than 60%, and the synthesis efficiency of the cyclic peptide can be greatly improved. The prepared cyclic peptide has high antibacterial activity. |