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

As natural-product-derived antibiotics, Desotamides A-D and wollamides exhibit growth inhibitory activity against Gram-posivite bacteria (IC50 0.6-7 μM) and are noncytotoxic to mammalian cells (IC50>30 μM). Herein we firstly report the total synthesis of above two cyclohexapeptides as well as a series of structural variants through solid phase peptide synthesis (SPPS), of which DE-3 displayed a 2-fold increase of anti-bacterial activity when compared with the original peptide DE-1. This strategy may offer good improvements for the synthesis of other cyclic peptides. This article is protected by copyright. All rights reserved.