Total Synthesis and Antibacterial Study of Cyclohexapeptides Desotamide B, Wollamide B and Their Analogs

Abstract

As natural‐product‐derived antibiotics, desotamides A – D and wollamides exhibit growth inhibitory activity against Gram ‐posivite bacteria ( IC 50 0.6 – 7 μ m ) and are noncytotoxic to mammalian cells ( IC 50 > 30 μ m ). Herein we firstly report the total synthesis of above two cyclohexapeptides as well as a series of structural variants through solid phase peptide synthesis, of which 3 displayed a 2‐fold increase of antibacterial activity when compared with the original peptide 1 . This strategy may offer good improvements for the synthesis of other cyclic peptides.