CHEMICAL MODIFICATION OF SPIRAMYCINS

VI. SYNTHESIS AND ANTIBACTERIAL ACTIVITIES OF 3, 3"-DI-O-ACYL- 4"-O-SULFONYL AND 3, 3"-DI-O-ACYL-4"-O-ALKYL DERIVATIVES OF SPIRAMYCIN I

抄録

3, 3"-Di-O-acyl-4"-O-sulfonyl and 3, 3"-di-O-acyl-4"-O-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-O-acetyl-4"-O-mesyl and 3, 3"-di-O-acetyl-4"-O-methylspiramycin I having relatively small substituents at 4"-position were the most effective in mouse protection tests, and the results were comparable to acetylspiramycin.