Chemical modification of spiramycins. IV. Synthesis and in vitro and in vivo activities of 3'',4''-diacylates and 3,3'',4''-triacylates of spriamycin I.
3'',4''-Diacylates and 3,3'',4''-triacylates of spiramycin I were synthesized and evaluated by the four parameters, MIC against bacteria, affinity to ribosomes, retention time in HPLC and therapeutic effect. Among them, 3,3'',4''-tri-O-propionyl and 3,4''-di-O-acetyl-3''-O-butyryl-spiramycin I were the most active in vivo, which were superior to acetylspiramycin.
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D007933:Leucomycins / Q000138:chemical synthesis*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008826:Microbial Sensitivity Tests; D012270:Ribosomes / Q000378:metabolism
D007933:Leucomycins