Abstract

Design and synthesis of conjugates consisting of the macrolide antibiotic desmycosin and fragments of the antibacterial peptide oncocin were performed in attempt to develop new antimicrobial compounds. New compounds were shown to bind to the E. coli 70S ribosomes, to inhibit bacterial protein synthesis in vitro, as well as to suppress bacterial growth. The conjugates of N-terminal hexa- and tripeptide fragments of oncocin and 3,2′,4′′-triacetyldesmycosin were found to be active against some strains of macrolide-resistant bacteria. By simulating molecular dynamics of the complexes of these compounds with the wild-type bacterial ribosomes and with ribosomes, containing A2059G 23S RNA mutation, the specific structural features of their interactions were revealed.

中文翻译：

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Desmycosin 与抗菌肽 Oncocin 片段的缀合物：合成、抗菌活性、与核糖体的相互作用

摘要

设计和合成由大环内酯类抗生素去霉素和抗菌肽癌素片段组成的缀合物，试图开发新的抗菌化合物。新化合物与大肠杆菌70S 核糖体结合，在体外抑制细菌蛋白质合成，以及抑制细菌生长。发现癌素的 N 端六肽和三肽片段与 3,2',4''-三乙酰去霉菌素的缀合物对某些大环内酯类耐药细菌菌株具有活性。通过模拟这些化合物与野生型细菌核糖体和含有 A2059G 23S RNA 突变的核糖体的复合物的分子动力学，揭示了它们相互作用的特定结构特征。