title: 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.
abstract: 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.
authors.affiliation: Sanraku Inc., Central Research Laboratories, Fujisawa, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Kiyoshima
authors.forename: M
authors.initials: M
authors.lastname: Sakamoto
authors.forename: H
authors.initials: H
authors.lastname: Nomura
authors.forename: T
authors.initials: T
authors.lastname: Yoshioka
authors.forename: R
authors.initials: R
authors.lastname: Okamoto
authors.forename: T
authors.initials: T
authors.lastname: Sawa
authors.forename: H
authors.initials: H
authors.lastname: Naganawa
authors.forename: T
authors.initials: T
authors.lastname: Takeuchi
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D015645:Tylosin