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  • Title: Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
    Author: Kobayashi Y, Ichioka M, Hirose T, Nagai K, Matsumoto A, Matsui H, Hanaki H, Masuma R, Takahashi Y, Omura S, Sunazuka T.
    Journal: Bioorg Med Chem Lett; 2010 Oct 15; 20(20):6116-20. PubMed ID: 20833545.
    Abstract:
    Novel bottromycin derivatives were synthesized from bottromycin A(2) via a hydrazide derivative as a common intermediate. Seventeen derivatives were subjected to in vitro evaluation against drug-resistant gram-positive bacteria. Some compounds showed potent anti-MRSA and anti-VRE activity, as did bottromycin A(2). Notably, a propyl ketone derivative exhibited good antibacterial activity with excellent metabolite stability.
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