Abstract
AbstractTo explore the structure‐activity relationships (SAR) of vancomycin and find more effective new chemical entities than known glycopeptides for the treatment of antibacterial infection, 11 novel vancomycin analogues 7 carrying N‐acyl‐substituted lipophilic substitutions on the vancosamine moiety and polar moieties on the seventh‐amino acid phenyl ring were designed and synthesized. These analogues 7 a–k have been evaluated in vitro for their antibacterial activities against S. epidermidis, S. aureus, E. faecalis and E. faecium (sensitive and resistant strains). Compounds 7 c, 7 f, and 7 i showed more potent antibacterial activity against S. aureus than vancomycin. In addition, compounds 7 f and 7 j showed promising antibacterial activity against sensitive S. epidermidis.
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