Solid-phase synthesis and antibacterial evaluations of N-demethylvancomycin derivatives.
Twenty-five N-demethylvancomycin derivatives were synthesized on solid-support and their structures were determined by LC-MS/MS. Biological evaluation of these compounds indicated that bulky hydrophobic substituent on vancosamine of N-demethylvancomycin can increase antibacterial activity against vancomycin-resistant Enterococcus faecalis.
Yao
Nian-Huan
NH
Chinese Academy of Medical Sciences & Peking Union Medical College, Institute of Materia Medica, 1 Xian Nong Tan Street, Beijing 100050, PR China.
Liu
Gang
G
He
Wen-Yi
WY
Niu
Changqun
C
Carlson
James R
JR
Lam
Kit S
KS
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D013293:Enterococcus faecalis / Q000187:drug effects; D007202:Indicators and Reagents; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D014640:Vancomycin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D007202:Indicators and Reagents; D014640:Vancomycin; C041572:N-demethylvancomycin