Application of the Suzuki–Miyaura cross-coupling to increase antimicrobial potency generates promising novel antibacterials

Antimicrobial peptides have been recognized as a novel class of antibiotics, and several candidates are currently in clinical trials. In this work, a tripeptide derivative containing 4-iodo phenylalanine has been derivatized through the Suzuki–Miyaura cross-coupling. This has enabled the rapid and efficient synthesis of an array of tripeptide derivatives encompassing novel biaryl moieties. The peptide derivatives show high activity against Gram-positive bacteria.