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-acetyl-3"-O-butyrylspiramycin I were the most active in viro, which were superior to acetylspiramycin.