Chemical modification of spiramycinsvi. synthesis and antibacterial activities of 3,3”-di-0-acyl-4“-o-sulfonyl and 3,3”-di-0-acyl-4 “-o-alkyl derivatives of spiramycin i

Abstract

3,3“-Di-O-acyl-4“-0-suIfonyl and 3,3“-di-0-acyl-4“-0-alkyl derivatives of spiramycin I were synthesized and evaluated by four parameters, antibacterial activity, affinity to ribosomes, lypophilicity and therapeutic effects. Among them, 3,3“-di-0-acetyl-4“-0-mesyl and 3,3“-di-0-acetyl-4“-0-methylspiramycin I having relatively small substituentsat 4“-position were the most effective in mouse protection tests, and the results were comparable to acetyl-spiramycin. © 1985, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.