Trifonova Zh P, Sturman N V, Katrukha G S, Fedorova G B
Antibiot Khimioter. 1988 Nov;33(11):814-7.
Various bifunctional reagents by the free NH2 group of ristomycinic acid of ristomycin A were used for selective chemical modification of the antibiotic. The bifunctional reagents were the following: di-N-hydroxysuccinimide ether of suberic acid and 4,4'-difluoro-3,3'-dinitrodiphenylsulfone. Bis-N,N'-derivatives of ristomycin A were prepared using these reagents. The derivatives inhibited the growth of Bac. subtilis but the concentrations required for the inhibition were 2-4 times higher than those of ristomycin A. It was noted that the MIC of the bis-N,N'-derivatives depended on the length and flexibility of the "binding foot". The MIC of the bis-N,N'-derivative prepared with using suberic acid was 2 times higher than that of the derivative prepared with the use of 4,4'-difluoro-3,3'-dinitrodiphenylsulfone.
利用多种双功能试剂通过瑞斯托菌素A的瑞斯托菌素酸的游离NH2基团对该抗生素进行选择性化学修饰。这些双功能试剂如下：辛二酸二-N-羟基琥珀酰亚胺醚和4,4'-二氟-3,3'-二硝基二苯砜。使用这些试剂制备了瑞斯托菌素A的双-N,N'-衍生物。这些衍生物抑制枯草芽孢杆菌的生长，但抑制所需浓度比瑞斯托菌素A高2至4倍。值得注意的是，双-N,N'-衍生物的最低抑菌浓度取决于“结合臂”的长度和柔韧性。用辛二酸制备的双-N,N'-衍生物的最低抑菌浓度比用4,4'-二氟-3,3'-二硝基二苯砜制备的衍生物高2倍。
