Tunicyclin D has been suggested to primarily target the fungal membrane,it is therefore difficult for fungal to develop resistance to this antibiotic because significant alterations of the fungal cell wall lipid composition would be required.[1-3] A series of glycosylated derivatives of Tunicyclin D were synthesized through a highly efficient and versatile synthetic method.The method is based on solid-phase peptide synthesis using 2-chlorotrityl resin as the solid-phase support and glycosyl amino acids as building blocks.Biological studies of the synthetic Tunicyclin D derivatives showed monosaccharide-containing compounds exhibit improved or similar antifungal activities,whereas the compounds carrying disaccharide glycans,showed much weaker antifungal activities.