Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives
作者:Hongjin Zhai、Chunying Luo、Pu Yang、Shuo Zhang、Huanhuan Wang、Yaquan Cao、Yingxue Yang、Haoyue Liu、Xiaoyan Kong、Firas Obald Arhema Frejat、Changzhong Ren、Xiufang Shi、Chunli Wu
DOI:10.1016/j.ejmech.2022.114495
日期:2022.8
antibiotics with excellent activity against drug-resistant bacteria. Three novel series of tylosin semisynthetic derivatives were designed, synthesized and evaluated for their antibacterial activities against various Gram-positive and Gram-negative bacteria. Among these derivatives, compound C-2 demonstrated potent antibacterial activity against both gram-positive and gram negative bacteria, and non mutagenic
随着抗生素耐药性的增加,迫切需要开发对耐药菌具有优异活性的新型抗生素。设计、合成了三个新型泰乐菌素半合成衍生物系列,并评估了它们对各种革兰氏阳性和革兰氏阴性细菌的抗菌活性。在这些衍生物中,化合物C-2对革兰氏阳性菌和革兰氏阴性菌均表现出有效的抗菌活性,且无致突变性。更重要的是,化合物C-2在小鼠模型中显示出对革兰氏阳性菌的高效抗菌效力,并且被发现比替地匹罗星更有效。因此,化合物C-2作为治疗细菌感染的有前途的先导化合物具有巨大的潜力。