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

Abstract

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-acetyI-3”-O-butyryl-spiramycin I were the most active in vivo, which were superior to acetylspiramycin. © 1984, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.