College of Pharmaceutical Sciences, Soochow University, 199 Ren-Ai Road, Suzhou 215123, China.
College of Chemistry and Environmental Engineering, Jiaozuo University, Ren-Min Road, Jiaozuo 454000, China.
Molecules. 2024 May 24;29(11):2492. doi: 10.3390/molecules29112492.
The development of antimicrobial drugs with novel structures and clear mechanisms of action that are active against drug-resistant bacteria has become an urgent need of safeguarding human health due to the rise of bacterial drug resistance. The discovery of AMPs and the development of amphipathic peptidomimetics have lay the foundation for novel antimicrobial agents to combat drug resistance due to their overall strong antimicrobial activities and unique membrane-active mechanisms. To break the limitation of AMPs, researchers have invested in great endeavors through various approaches in the past years. This review summarized the recent advances including the development of antibacterial small molecule peptidomimetics and peptide-mimic cationic oligomers/polymers, as well as mechanism-of-action studies. As this exciting interdisciplinary field is continuously expanding and growing, we hope this review will benefit researchers in the rational design of novel antimicrobial peptidomimetics in the future.
由于细菌耐药性的出现，开发具有新型结构和明确作用机制、对耐药菌有效的抗菌药物已成为保障人类健康的迫切需要。抗菌肽的发现和两亲性肽模拟物的发展为新型抗菌药物的开发奠定了基础，因为它们具有全面的强大抗菌活性和独特的膜活性机制。为了克服抗菌肽的局限性，研究人员在过去几年中通过各种方法投入了大量的努力。本综述总结了近年来的进展，包括抗菌小分子肽模拟物和肽模拟阳离子低聚物/聚合物的开发，以及作用机制的研究。随着这一令人兴奋的跨学科领域的不断扩展和发展，我们希望本综述将有助于未来研究人员合理设计新型抗菌肽模拟物。
