Sano H, Sunazuka T, Tanaka H, Yamashita K, Okachi R, Omura S
J Antibiot (Tokyo). 1984 Jul;37(7):750-9. doi: 10.7164/antibiotics.37.750.
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.
在螺旋霉素I的叔丁基二甲基硅醚保护的衍生物中，发现2'-O-乙酰螺旋霉素I 3,18-(O-叔丁基二甲基硅基)缩醛是螺旋霉素I 4''-修饰的合适中间体。合成了7种4''-磺酸盐和4种4''-烷基醚，它们在体外对细菌的活性比螺旋霉素I更高。具有相对较小磺酰基和烷基的4''-取代衍生物在治疗效果上与螺旋霉素I相当。
