Seneci P, Trani A, Ferrari P, Scotti R, Ciabatti R
Marion Merrell Dow Research Institute, Lepetit Research Center, Gerenzano (VA), Italy.
J Antibiot (Tokyo). 1992 Oct;45(10):1633-44. doi: 10.7164/antibiotics.45.1633.
A series of O56-substituted carboxyester or carboxyamide derivatives of deglucoteicoplanin (TD) was prepared by condensation of the 56-hydroxyl function with various alkylating agents of general formula RBr, where R represents functional groups with different physico-chemical properties. The modifications at position 56 influenced the antimicrobial activity of the new derivatives; activity depended on the structure of various R groups, their ionic properties, and their steric hindrance. The activity of the new compounds did not show any significant improvement when compared with TD. The physico-chemical and antibacterial properties of the synthesized compounds are reported.
通过将去糖替考拉宁（TD）的56-羟基官能团与通式为RBr的各种烷基化剂缩合，制备了一系列O56-取代的去糖替考拉宁羧基酯或羧基酰胺衍生物，其中R代表具有不同物理化学性质的官能团。56位的修饰影响了新衍生物的抗菌活性；活性取决于各种R基团的结构、它们的离子性质和空间位阻。与TD相比，新化合物的活性没有显示出任何显著提高。报道了合成化合物的物理化学和抗菌性能。
