The emergence of multirresistant pathogens, even to last-resort antimicrobials and phytosanitaries, can seriously endanger human health and food security, and therefore, WHO and FAO have asked for urgent actions to address this threat. Among the new antimicrobials, host-defense peptides are particularly promising, since they display a broad activity spectrum but with a very low induction of resistance. Another promising strategy is the development of quorum quenchers, molecules which interfere with the bacterial communication systems that are involved in virulence, coordinated invasion of the host, generation of biofilms, etc. In this communication, the selective modification of amino acid and peptides using “customizable units” will be applied to the preparation of potential antimicrobial peptides and quorum quenchers. The Scheme shows that a starting peptide with two different customizable units (Ser and Hyp) can be selectively modified, allowing the preparation of peptides “à la carte”, with different α-chains and N-substituents.

Site-selective modification of peptides for the production of libraries of potential antimicrobial and quorum quencher compounds

ACS Spring Meeting 2021

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