The main achievements in the development of methods for the design of semisynthetic antibiotics of a new generation belonging to the group of polycyclic glycopeptides directed against infections caused by multidrug-resistant bacteria and dangerous human and animal viruses are reviewed. The review is focused on the results obtained at the Gauze Institute in the area of chemical modification of natural antibiotics (eremomycin, vancomycin, teicoplanin, etc.) directed toward modification of their antibacterial and/or antiviral activity. A special emphasis is placed on the study of the mechanisms of action of these antibiotics, which could be the basis of a rational approach to their chemical modification involving the transformation of the inner binding pocket and the peripheral regions of the molecules that participate in the formation of their complexes with targets. The recently discovered antiviral activity of modified glycopeptides antibiotics is also discussed. A possibility of obtaining new highly active anti-HIV-1 and anti-HIV-2 preparations on the basis of hydrophobic derivatives of the aglycones of glycopeptide antibiotics was demonstrated. New semisynthetic derivatives of antibiotics that exhibit a high antibacterial activity in vivo, have good pharmacological characteristics, and are promising for practical use are described.

中文翻译：

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一系列半合成多环糖肽抗生素的构效关系


综述了针对多重耐药细菌和危险的人类和动物病毒引起的感染的新一代多环糖肽类半合成抗生素设计方法的主要成就。该审查的重点是纱布研究所在天然抗生素（埃雷霉素、万古霉素、替考拉宁等）化学修饰领域获得的结果，旨在修饰其抗菌和/或抗病毒活性。特别强调这些抗生素的作用机制的研究，这可能是对其化学修饰的合理方法的基础，涉及内部结合袋和参与形成的分子的外围区域的转化他们与目标的复合体。还讨论了最近发现的修饰糖肽抗生素的抗病毒活性。证明了基于糖肽抗生素苷元的疏水性衍生物获得新的高活性抗HIV-1和抗HIV-2制剂的可能性。描述了新的抗生素半合成衍生物，它们在体内表现出高抗菌活性，具有良好的药理特性，并且具有实际应用前景。