Bottromycin derivatives: Efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities |
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| Authors: | Yutaka Kobayashi Maki Ichioka Tomoyasu Hirose Kenichiro Nagai Atsuko Matsumoto Hidehiro Matsui Hideaki Hanaki Rokuro Masuma Yoko Takahashi Satoshi Ōmura Toshiaki Sunazuka |
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| Affiliation: | Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan |
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| Abstract: | Novel bottromycin derivatives were synthesized from bottromycin A2 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 A2. Notably, a propyl ketone derivative exhibited good antibacterial activity with excellent metabolite stability. |
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