Sano H, Tanaka H, Yamashita K, Okachi R, Omura S
J Antibiot (Tokyo). 1985 Feb;38(2):186-96. doi: 10.7164/antibiotics.38.186.
The 3'- and 4''-de-N-methylspiramycins were synthesized selectively, and then were converted to various N-substituted derivatives. 4''-De-N-methyl derivatives were more active than 3'-de-N-methyl ones. Among the derivatives, 4''-N-Fmoc-glycyl and 4''-N-benzyl-4''-de-N-methylspiramycin I were the most active in vitro, and were comparable to spiramycin I. 4''-De-N-methylspiramycin I was about half as active as spiramycin I in vivo.
选择性合成了3'-和4''-去N-甲基螺旋霉素，然后将它们转化为各种N-取代衍生物。4''-去N-甲基衍生物比3'-去N-甲基衍生物更具活性。在这些衍生物中，4''-N-芴甲氧羰基-甘氨酰基和4''-N-苄基-4''-去N-甲基螺旋霉素I在体外活性最高，与螺旋霉素I相当。4''-去N-甲基螺旋霉素I在体内的活性约为螺旋霉素I的一半。
