title: Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
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.
authors.affiliation: Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato University, Tokyo, Japan.
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Kobayashi
authors.forename: Maki
authors.initials: M
authors.lastname: Ichioka
authors.forename: Tomoyasu
authors.initials: T
authors.lastname: Hirose
authors.forename: Kenichiro
authors.initials: K
authors.lastname: Nagai
authors.forename: Atsuko
authors.initials: A
authors.lastname: Matsumoto
authors.forename: Hidehiro
authors.initials: H
authors.lastname: Matsui
authors.forename: Hideaki
authors.initials: H
authors.lastname: Hanaki
authors.forename: Rokuro
authors.initials: R
authors.lastname: Masuma
authors.forename: Yoko
authors.initials: Y
authors.lastname: Takahashi
authors.forename: Satoshi
authors.initials: S
authors.lastname: Omura
authors.forename: Toshiaki
authors.initials: T
authors.lastname: Sunazuka
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial; D056569:Enterococcaceae / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy; D006801:Humans; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D051379:Mice; D008826:Microbial Sensitivity Tests; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D010949:Plasma / Q000378:metabolism; D014640:Vancomycin / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D010456:Peptides, Cyclic; C012218:bottromycin A(2); D014640:Vancomycin