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

K Kiyoshima; M Sakamoto; H Nomura; T Yoshioka; R Okamoto; T Sawa; H Naganawa; T Takeuchi

doi:10.7164/antibiotics.42.1661

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

J Antibiot (Tokyo). 1989 Nov;42(11):1661-72. doi: 10.7164/antibiotics.42.1661.

Authors

K Kiyoshima¹, M Sakamoto, H Nomura, T Yoshioka, R Okamoto, T Sawa, H Naganawa, T Takeuchi

Affiliation

¹ Sanraku Inc., Central Research Laboratories, Fujisawa, Japan.

PMID: 2584151
DOI: 10.7164/antibiotics.42.1661

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.

Publication types

Comparative Study

MeSH terms

Anti-Bacterial Agents / pharmacology
Drug Resistance, Microbial
Microbial Sensitivity Tests
Molecular Structure
Mycoplasma / drug effects*
Staphylococcus / drug effects*
Structure-Activity Relationship
Tylosin / analogs & derivatives*
Tylosin / pharmacology

Substances

Anti-Bacterial Agents
Tylosin