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Comparative Study
. 1985 Jul:16 Suppl A:1-11.
doi: 10.1093/jac/16.suppl_a.1.

Structure activity relationships of spiramycins

S Omura, H Sano, T Sunazuka
Comparative Study

Structure activity relationships of spiramycins

S Omura et al. J Antimicrob Chemother. 1985 Jul.

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.

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