Mojsoska Biljana
Department of Science and Environment, Roskilde University, Denmark.
Methods Enzymol. 2022;663:327-340. doi: 10.1016/bs.mie.2021.10.010. Epub 2021 Dec 7.
Bacterial resistance to conventional antibiotics poses an immense threat to human health and consequently many bacterial infections arise from multi-drug resistant pathogens. It is, therefore, necessary to continue to develop novel antimicrobials. Peptoids are a novel class of antimicrobial agents that mimic the structures of peptides. These N-substituted glycines differ from peptides in the side chain attachment site where in peptoids, the side chain functionality is introduced at the nitrogen rather than the α-carbon in peptides. During the process of design and development of antimicrobial peptoids, several key elements such as charge and amphiphilicity appear to guide peptoid bioactivity against bacterial pathogens. In this study, we report a quick synthesis of three novel cationic antimicrobial peptoids that contain charged, hydrophobic, and chiral monomers. This study is the first to use a monomer that contains both charge and chiral center for the design of the novel peptoid sequences.
细菌对传统抗生素的耐药性对人类健康构成了巨大威胁，因此许多细菌感染是由多重耐药病原体引起的。因此，有必要继续开发新型抗菌药物。类肽是一类新型抗菌剂，可模拟肽的结构。这些N-取代甘氨酸与肽在侧链连接位点不同，在类肽中，侧链官能团是在氮原子上引入的，而不是在肽的α-碳原子上。在抗菌类肽的设计和开发过程中，几个关键要素如电荷和两亲性似乎指导着类肽对细菌病原体的生物活性。在本研究中，我们报告了三种新型阳离子抗菌类肽的快速合成，这些类肽含有带电荷、疏水和手性单体。本研究首次使用同时含有电荷和手性中心的单体来设计新型类肽序列。
