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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.

journal of antibiotics

Chemical modification of spiramycins. IV. Synthesis and in vitro and in vivo activities of 3", 4"-diacylates and 3, 3" ,4"-triacylates of spiramycin I.