The emergence of drug-resistant bacteria has led to the high demand for new antibiotics. In this report, we investigated membrane-active antimicrobial β-cyclodextrins. These contain seven amino-modified alkyl groups on a molecule, which act as functional moieties to permeabilize bacterial cell membranes. The polyfunctionalization of cyclodextrins was achieved through a click reaction assisted by microwave irradiation. A survey using derivatives with systematically varied functionalities clarified the unique correlation of the antimicrobial activity of these compounds with their molecular structure and hydrophobicity/hydrophilicity balances. The optimum hydrophobicity for the compounds being membrane-active was specific to bacterial strains and animal cells; this led to specific compounds having selective toxicity against bacteria including multidrug-resistant pathogens. The results demonstrate that cyclodextrin is a versatile molecular scaffold for rationally designed structures and can be used for the development of new antibiotics.

中文翻译：

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通过点击反应 合成的膜活性抗菌聚（氨基修饰的烷基）β-环糊精†

耐药细菌的出现导致了对新抗生素的高需求。在本报告中，我们研究了膜活性抗菌素β-环糊精。它们在分子上包含七个氨基修饰的烷基，它们充当使细菌细胞膜通透的功能性部分。环糊精的多官能化是通过微波辐射辅助的点击反应实现的。使用具有系统变化的功能的衍生物进行的一项调查阐明了这些化合物的抗菌活性与其分子结构和疏水性/亲水性平衡之间的独特关联。具有膜活性的化合物的最佳疏水性是细菌菌株和动物细胞所特有的。这导致特定的化合物对细菌（包括耐多药病原体）具有选择性毒性。结果表明，环糊精是用于合理设计结构的通用分子支架，可用于开发新的抗生素。