{"title":"OBOC screening of high activity and low-toxic polymyxin analogs against MCR-1 resistant strains.","authors":"Wenhong Zheng, Xin Wang, Hao Lian, Pengfei Zou, Tongyi Sun, Hao Wang, Li-Li Li","doi":"10.1039/d5bm00362h","DOIUrl":null,"url":null,"abstract":"<p><p>We performed inverse synthesis to create 1152 structural analogs of polymyxin B with modified hydrophilicity and charge properties using OBOC technology. This led to the identification of two promising candidates that provided insights into structure-activity relationships. These compounds maintained high antibacterial activity while expanding the safety window 4-16 times.</p>","PeriodicalId":65,"journal":{"name":"Biomaterials Science","volume":" ","pages":""},"PeriodicalIF":5.8000,"publicationDate":"2025-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Biomaterials Science","FirstCategoryId":"5","ListUrlMain":"https://doi.org/10.1039/d5bm00362h","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"MATERIALS SCIENCE, BIOMATERIALS","Score":null,"Total":0}
引用次数: 0
Abstract
We performed inverse synthesis to create 1152 structural analogs of polymyxin B with modified hydrophilicity and charge properties using OBOC technology. This led to the identification of two promising candidates that provided insights into structure-activity relationships. These compounds maintained high antibacterial activity while expanding the safety window 4-16 times.
期刊介绍:
Biomaterials Science is an international high impact journal exploring the science of biomaterials and their translation towards clinical use. Its scope encompasses new concepts in biomaterials design, studies into the interaction of biomaterials with the body, and the use of materials to answer fundamental biological questions.