Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors

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• 作者：Truong Thanh Tung^a ; Tim Holm Jakobsen^b ; Trong Tuan Dao^a ; ^c ; Anja Thoe Fuglsang^c ; Michael Givskov^b ; ^d ; Sø ; ren Brø ; gger Christensen^a ; ^{soren.christensen@sund.ku.dk} ; John Nielsen^a ; ^{john.nielsen@sund.ku.dk}
• 关键词：Fusaric acid ; Quorum sensing inhibitors ; Microwave-assisted synthesis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：1011-1020
• 全文大小：1274 K
• 卷排序：126

文摘

40 novel FA analogues were prepared efficiently by microwave-assisted synthesis. Fusaric acid is bioequivalent with the endogenous QS signal molecules. Natural product scaffolds as a starting point for developing QSIs. Eight compounds inhibit lux QS system and one compound inhibit las QS system. Structure-activity relationships have been established.