CHEMICAL MODIFICATION OF SPIRAMYCINS

III. SYNTHESIS AND ANTIBACTERIAL ACTIVITIES OF 4"-SULFONATES AND 4"-ALKYLETHERS OF SPIRAMYCIN I

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Among the derivatives protected with t-butyldimethylsilylether of spiramycin I, 2'-O-acetylspiramycin I 3, 18-(O-t-butyldimethylsilyl)acetal was found to be a suitable intermediate for 4"-modification of spiramycin I. Seven 4"-sulfonates and four 4"-alkylethers were synthesized, which were more active against bacteria in vitro than spiramycin I. 4"-Substituted derivatives with relatively small sulfonyl and alkyl groups were comparable in therapeutic effect to spiramycin I.