Design, synthesis, and evaluation of efflux substrate-metal chelator conjugates as potential antimicrobial agents

作者：Zheng Yanling; Ballard C Eric; Zheng Shi Long; Gao Xingming; Ko Ko Chun; Yang Hsiuchin; Brandt Gary; Lou Xinhui; Tai Phang C; Lu Chung Dar; Wang Binghe^*

来源：Bioorganic & Medicinal Chemistry Letters, 2007, 17(3): 707-711.

DOI：10.1016/j.bmcl.2006.10.094

• design
• synthesis
• efflux substrate-metal chelator conjugates
• antimicrobial agents

Maintaining a proper balance of metal concentrations is critical to the survival of bacteria. We have designed and synthesized a series of conjugates of metal chelators and efflux transporter substrates aimed at disrupting bacterial metal homeostasis to achieve bacterial killing. Biological studies showed that two of the compounds had very significant antimicrobial effect with an MIC value of 7.8 mu g/mL against Gram-positive Bacillus subtilis.

• 出版日期2007-2-1