Antibacterial activity of G6-quaternary ammonium derivatives of a lipophilic vancomycin analogue.
A series of G6-amino derivatives of a lipophilic vancomycin analogue was prepared. Antibacterial activity of the analogues was inversely proportional to the degree of substitution of the G6-nitrogen. The fully substituted (quaternary) analogues were essentially inactive against vanA phenotype VREF strains but retained substantial activity against other bacteria, a profile reminiscent of teicoplanin.
Blizzard
Timothy A
TA
Merck Research Laboratories, RY800-B116, PO Box 2000, Rahway, NJ 07065, USA. tim_blizzard@merck.com
Kim
Ronald M
RM
Morgan
Jerry D
JD
Chang
Jiang
J
Kohler
Joyce
J
Kilburn
Ruth
R
Chapman
Kevin
K
Hammond
Milton L
ML
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004351:Drug Resistance; D057927:Hydrophobic and Hydrophilic Interactions; D008826:Microbial Sensitivity Tests; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013291:Streptococcus / Q000187:drug effects; D013329:Structure-Activity Relationship; D014640:Vancomycin / Q000031:analogs & derivatives*
D000900:Anti-Bacterial Agents; D000644:Quaternary Ammonium Compounds; D014640:Vancomycin