Novel semi-synthetic glycopeptide antibiotics active against methicillin-resistant staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE): doubly-modified water-soluble derivatives of chloroorienticin B.
A series of N-alkylated and aminomethylated derivatives of chloroorienticin B, a vancomycin-related glycopeptide antibiotic, were synthesized. Doubly-modified derivatives having both hydrophobic and hydrophilic substituents exhibited potent antibacterial activity against MRSA and VRE along with considerable water-solubility.
Yoshida
Osamu
O
Discovery Research Laboratories, Shionogi & Co., Ltd., Sagisu 5-12-4, Fukushima-ku, 553-0002, Osaka, Japan.
Yasukata
Tatsuro
T
Sumino
Yukihito
Y
Munekage
Tadashi
T
Narukawa
Yukitoshi
Y
Nishitani
Yasuhiro
Y
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016983:Enterococcus / Q000187:drug effects*; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D012995:Solubility; D013211:Staphylococcus aureus / Q000187:drug effects*; D014640:Vancomycin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020713:Vancomycin Resistance
D000900:Anti-Bacterial Agents; C057894:chloroorienticin B; D014640:Vancomycin