Structure activity relationships of spiramycins

descriptionPublicationkeyboard_double_arrow_right Article 01 Jan 1985 English Publisher:Oxford University Press (OUP)Journal:Journal of Antimicrobial Chemotherapy, volume 16, pages 1-11 (issn: 0305-7453, eissn: 1460-2091,

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Authors: S, Omura; H, Sano; T, Sunazuka;

doi: 10.1093/jac/16.suppl_a.1

pmid: 3902764

Structure activity relationships of spiramycins

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Abstract

Sixty-six derivatives of spiramycin I and neospiramycin I were synthesized and evaluated by four parameters, MIC, affinity to ribosomes (ID50), therapeutic effect in mice and retention time in HPLC. Among the derivatives, 3,3'',4''-tri-O-propionyl- and 3,4''-di-O-acetyl-3''-O-butyrylspiramycin I showed the highest therapeutic effect which was superior to acetylspiramycin. Structure activity relationships of spiramycins are discussed.

Related Organizations

Kitasato University
Japan

Keywords

Mice, Structure-Activity Relationship, Escherichia coli, Animals, Microbial Sensitivity Tests, Leucomycins, Ribosomes, Chromatography, High Pressure Liquid

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