Department of Pharmacy, Epigenetic Medicinal Chemistry Laboratory, University of Salerno , Fisciano, Italy.
Expert Opin Ther Pat. 2020 Dec;30(12):911-915. doi: 10.1080/13543776.2020.1822818. Epub 2020 Sep 20.
The insurgence of antibiotic resistance represents one of the biggest public health challenges of our times. During the years, different compounds were developed to fight against resistant bacterial cells, exploiting different mechanisms of action.
The patent application describes a set of antimicrobial compounds bearing to the class of the conjugated oligoelectrolytes (COEs). These are molecules characterized by hydrophobic conjugated backbone and terminal polar ionic pendants, able to intercalate into lipid bilayers of bacterial cells. The patent reports the preparation of 15 new compounds and the evaluation of their antimicrobial effect against ESKAPE pathogens ( .).
The preparation of the compounds claimed is simple and the preliminary activity data are very interesting. Among the claimed compounds, and have the ability to strongly inhibit the bacterial growth at doses similar to the ones of last resource antibiotics. Unfortunately, no in-vivo data are reported. Moreover, the presence of several quaternary amines limits the potential application of these compounds only to topical uses.
抗生素耐药性的出现是我们这个时代最大的公共卫生挑战之一。多年来，人们开发了不同的化合物来对抗耐药细菌细胞，利用不同的作用机制。
该专利申请描述了一组带有共轭低聚物（COEs）类别的抗菌化合物。这些分子的特点是具有疏水性共轭主链和末端极性离子侧链，可以插入细菌细胞膜的脂质双层中。该专利报告了 15 种新化合物的制备及其对 ESKAPE 病原体（ .）的抗菌效果评价。
所要求化合物的制备简单，初步活性数据非常有趣。在所要求的化合物中， 和 具有在类似于最后资源抗生素剂量下强烈抑制细菌生长的能力。不幸的是，没有报告体内数据。此外，由于存在几个季铵盐，这些化合物的潜在应用仅限于局部使用。
