Design, Synthesis, and Biological Evaluation of Hexacyclic Tetracyclines as Potent, Broad Spectrum Antibacterial Agents

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• 作者：Cuixiang Sun ; Diana K. Hunt ; Chi-Li Chen ; Yonghong Deng ; Minsheng He ; Roger B. Clark ; Corey Fyfe ; Trudy H. Grossman ; Joyce A. Sutcliffe ; Xiao-Yi Xiao
• 刊名：Journal of Medicinal Chemistry
• 出版年：2015
• 出版时间：June 11, 2015
• 年：2015
• 卷：58
• 期：11
• 页码：4703-4712
• 全文大小：475K
• ISSN：1520-4804

文摘

A series of novel hexacyclic tetracycline analogues (鈥渉exacyclines鈥? was designed, synthesized, and evaluated for antibacterial activity against a wide range of clinically important bacteria isolates, including multidrug-resistant, Gram-negative pathogens. Valuable structure鈥揳ctivity relationships were identified, and several hexacyclines displayed potent, broad spectrum antibacterial activity, including promising anti-Pseudomonas aeruginosa activity in vitro and in vivo.