Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
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.
Kobayashi
Yutaka
Y
Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato University, Tokyo, Japan.
Ichioka
Maki
M
Hirose
Tomoyasu
T
Nagai
Kenichiro
K
Matsumoto
Atsuko
A
Matsui
Hidehiro
H
Hanaki
Hideaki
H
Masuma
Rokuro
R
Takahashi
Yoko
Y
Omura
Satoshi
S
Sunazuka
Toshiaki
T
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
D000900:Anti-Bacterial Agents; D010456:Peptides, Cyclic; C012218:bottromycin A(2); D014640:Vancomycin