CHEMICAL MODIFICATION OF SPIRAMYCINS

I. SYNTHESIS OF THE ACETAL DERIVATIVES OF NEOSPIRAMYCIN I

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Tetrahydrofuranyl and tetrahydropyranyl derivatives of neospiramycin I at 3 and/or 4' position were synthesized. In vitro and in vivo activities of these derivatives were correlated with the position and configuration of acetal groups. The most effective derivative, 3-a, 4'-a-di-O-tetrahydrofuranylneospiramycin I was comparable to spiramycin I.