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Teixobactin represents a new class of antibiotics with novel structure and excellent activity against Gram-positive pathogens and  Mycobacterium tuberculosis . Herein, we report a one-pot reaction to conveniently construct the key building block  l -allo-Enduracidine in 30-gram scale in just one hour  and a convergent strategy (3 + 2 + 6) to accomplish a gram-scale total synthesis of teixobactin. Several analogs are described, with  20  and  26  identified as the most efficacious analogs with 3~8-fold and 2~4-fold greater potency against vancomycin resistant  Enterococcus faecalis  and methicillin-resistant  Staphylococcus aureus  respectively in comparison with teixobactin. In addition, they show high efficiency in  Streptococcus pneumoniae  septicemia mouse model and neutropenic mouse thigh infection model using methicillin-resistant  Staphylococcus aureus . We also propose that the antiparallel β-sheet of teixobactin is important for its bioactivity and an antiparallel dimer of teixobactin is the minimal binding unit for lipid II via key amino acids variations and molecular docking.

Gram-scale total synthesis of teixobactin promoting binding mode study and discovery of more potent antibiotics