细菌
合理设计
阳离子聚合
两亲性
抗菌剂
膜
化学
革兰氏阴性菌
革兰氏阳性菌
生物物理学
组合化学
生物化学
生物
大肠杆菌
纳米技术
有机化学
材料科学
聚合物
共聚物
基因
遗传学
作者
Alysha Moretti,Richard Weeks,Michael L. Chikindas,Kathryn E. Uhrich
出处
期刊:Langmuir
[American Chemical Society]
日期:2019-03-19
卷期号:35 (16): 5557-5567
被引量:15
标识
DOI:10.1021/acs.langmuir.9b00110
摘要
Small-molecule cationic amphiphiles (CAms) were designed to combat the rapid rise in drug-resistant bacteria. CAms were designed to target and compromise the structural integrity of bacteria membranes, leading to cell rupture and death. Discrete structural features of CAms were varied, and structure–activity relationship studies were performed to guide the rational design of potent antimicrobials with desirable selectivity and cytocompatibility profiles. In particular, the effects of cationic conformational flexibility, hydrophobic domain flexibility, and hydrophobic domain architecture were evaluated. Their influence on antimicrobial efficacy in Gram-positive and Gram-negative bacteria was determined, and their safety profiles were established by assessing their impact on mammalian cells. All CAms have a potent activity against bacteria, and hydrophobic domain rigidity and branched architecture contribute to specificity. The insights gained from this project will aid in the optimization of CAm structures.
科研通智能强力驱动
Strongly Powered by AbleSci AI