Structure-activity relationships and optimization of acyclic acylphloroglucinol analogues as novel antimicrobial agents

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• 作者：Haibo Tan^a ; ¹ ; Hongxin Liu^a ; ^b ; ¹ ; Liyun Zhao^a ; ^c ; Yao Yuan^a ; ^c ; Bailin Li^a ; ^c ; Yueming Jiang^a ; Liang Gong^a ; ^{lianggong@scbg.ac.cn} ; Shengxiang Qiu^a ; ^{sxqiu@scbg.ac.cn}
• 关键词：Anti-MRSA ; Acylphloroglucinol ; Mechanism ; Structure-activity relationship
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：492-499
• 全文大小：985 K
• 卷排序：125

文摘

Twenty one acylphloroglucinols possessing different side chains were synthesized. An unambiguous structure-activity relationship towards anti-MRSA was revealed. Compound 11j was identified as a very promising lead compound. 11j included membrane depolarization and, to a lesser extent, membrane disruption.