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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. 1989
K Kiyoshima, and
M Sakamoto, and
H Nomura, and
T Yoshioka, and
R Okamoto, and
T Sawa, and
H Naganawa, and
T Takeuchi
Sanraku Inc., Central Research Laboratories, Fujisawa, Japan.
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.
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