期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 135, 期 8, 页码 2927-2930出版社
AMER CHEMICAL SOC
DOI: 10.1021/ja3120955
关键词
-
资金
- German Academy of Sciences Leopoldina [LPDS 2009-45]
- Human Frontier Science Program LTF Fellowship
- NIH [GM086258, GM18568, GM82137, GM58213]
- NERCE-BEID [5U54 AI057159]
- NIAID [P01AI083214]
- BASF
Biofilms are often associated with human bacterial infections, and the natural tolerance of biofilms to antibiotics challenges treatment. Compounds with anti-biofilm activity could become useful adjuncts to antibiotic therapy. We used norspermidine, a natural trigger for biofilm disassembly in the developmental cycle of Bacillus subtilis, to develop guanidine and biguanide compounds with up to 20-fold increased potency in preventing biofilm formation and breaking down existing biofilms. These compounds also were active against pathogenic Staphylococcus aureus. An integrated approach involving structure activity relationships, protonation constants, and crystal structure data on a focused synthetic library revealed that precise spacing of positively charged groups and the total charge at physiological pH distinguish potent biofilm inhibitors.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据