Synthesis of rigidly-linked vancomycin dimers and their in vivo efficacy against resistant bacteria.
A novel and efficient avenue for the preparation of dimeric vancomycins is described, and the dimers exhibited excellent antibacterial activities in the murine infection model.
Lu
Jun
J
Department of Chemistry, Graduate School of Science, Nagoya University, Chikusa, Nagoya, 464-8602, Japan.
Yoshida
Osamu
O
Hayashi
Sayaka
S
Arimoto
Hirokazu
H
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D003432:Cross-Linking Reagents / Q000737:chemistry*; D019281:Dimerization; D004195:Disease Models, Animal; D013293:Enterococcus faecalis / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D010078:Oxazines / Q000737:chemistry; D011008:Pneumococcal Infections / Q000188:drug therapy / Q000382:microbiology; D011014:Pneumonia / Q000188:drug therapy / Q000382:microbiology; D013211:Staphylococcus aureus / Q000187:drug effects; D013296:Streptococcus pneumoniae / Q000187:drug effects / Q000502:physiology; D014640:Vancomycin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D020713:Vancomycin Resistance / Q000187:drug effects*
D000900:Anti-Bacterial Agents; D003432:Cross-Linking Reagents; D010078:Oxazines; C006401:actinocin; D014640:Vancomycin