Structure activity relationships of spiramycins.
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.
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004926:Escherichia coli / Q000378:metabolism; D007933:Leucomycins / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D051379:Mice; D008826:Microbial Sensitivity Tests; D012270:Ribosomes / Q000378:metabolism; D013329:Structure-Activity Relationship
D007933:Leucomycins