Structure-activity relationship studies on 4''-O-acyltylosin derivatives: significance of their 23-O-mycinosyl and 4''-O-acyl moieties in antimicrobial activity against macrolide-resistant microbes.
Essential roles for both the 23-O-mycinosyl and 4''-O-acyl moieties of 4''-O-acyltylosin derivatives in the expression of antimicrobial activity against multiple macrolide-resistant strains of Staphylococci and mycoplasmas were demonstrated by in vitro comparison of the MICs of erythromycin, josamycin, tylosin and its 3- and 4''-O-acyl derivatives, demycinosyltylosin (DMT) and its 3- and 4''-O-acyl derivatives and 23-modified 3-O-acetyl-4''-O-isovaleryl-DMT derivatives.
Kiyoshima
K
K
Sanraku Inc., Central Research Laboratories, Fujisawa, Japan.
Sakamoto
M
M
Nomura
H
H
Yoshioka
T
T
Okamoto
R
R
Sawa
T
T
Naganawa
H
H
Takeuchi
T
T
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D004352:Drug Resistance, Microbial; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009174:Mycoplasma / Q000187:drug effects*; D013210:Staphylococcus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D015645:Tylosin / Q000031:analogs & derivatives* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D015645:Tylosin