Not only is the total synthesis and evaluation of key analogs of vancomycin with single atom changes in the binding pocket disclosed, but also their peripherals exemplified by N-4- (4'-chlorobiphenyl) -methyl derivatives Modified N- (hydrophobic substituted) derivatives and their pharmaceutically acceptable salts are disclosed. Their evaluation shows that the combination of pocket analogs and peripherally modified analogs has a prominent spectrum of antibacterial activity against both vancomycin-sensitive and vancomycin-resistant bacteria and truly touching potency, and perhaps two independent Directing to show benefits from a synergistic mechanism of action. A pharmaceutical composition containing a contemplated compound or a pharmaceutically acceptable salt thereof is obtained by administering an antibacterial amount of a contemplated compound or salt thereof as described above to an infected mammal in need of treatment. As a method of treating bacterial infections. [Selection figure] None
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