Application of two orthogonal click-type reactions for the preparation of cyclic peptides with antibacterial and anticancer activity

Abstract

The increase of antibiotic resistance gives rise to the urgent need for new antibiotics. One interesting approach to overcome this issue is the use of antimicrobial peptides. In this PhD thesis, we present the development of a new synthetic strategy for the preparation of amphiphilic cyclic peptides with potential antimicrobial properties. In this regard, we design a versatile peptidic platform that can be modified to obtain a library of different peptides. Several modifications have been performed to improve the bactericidal activity as well as to decrease the toxic side effects. The most potent cyclic peptides also shown promising activity against mature biofilm. Dox-bioconjugation provides a new strategy for cell delivery.