Pavlov A Y, Preobrazhenskaya M N, Malabarba A, Ciabatti R, Colombo L
Institute of New Antibiotics, Russian Academy of Medical Sciences, Moscow, Russia.
J Antibiot (Tokyo). 1998 Jan;51(1):73-8. doi: 10.7164/antibiotics.51.73.
A series of 7d-aminomethylated derivatives (mono modified) and their amides (double modified) at the amino acid No. 7 of teicoplanin aglycon were prepared with the aim of obtaining activity against vancomycin-resistant VanA enterococci. Among mono modified compounds, the 7d-n-decylaminomethyl derivative was the most active against VanA enterococci (4 micrograms/ml). Amides of the latter with 3-dimethylamino-propylamine or methylamine were found to be up to four times more active against glycopeptide-susceptible Gram-positive bacteria, and up to four times less active against VanA enterococci than the starting compound.
制备了一系列替考拉宁苷元第7位氨基酸的7-氨基甲基化衍生物（单修饰）及其酰胺（双修饰），目的是获得针对耐万古霉素的VanA肠球菌的活性。在单修饰化合物中，7-正癸基氨基甲基衍生物对VanA肠球菌的活性最高（4微克/毫升）。发现后者与3-二甲基氨基丙胺或甲胺形成的酰胺对糖肽敏感的革兰氏阳性菌的活性提高了四倍，而对VanA肠球菌的活性比起始化合物低四倍。
