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. 2017 Jan 27:126:1011-1020.
doi: 10.1016/j.ejmech.2016.11.044. Epub 2016 Nov 24.

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

Truong Thanh Tung  1 , Tim Holm Jakobsen  2 , Trong Tuan Dao  3 , Anja Thoe Fuglsang  4 , Michael Givskov  5 , Søren Brøgger Christensen  6 , John Nielsen  7
Affiliations

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

Truong Thanh Tung et al. Eur J Med Chem. .

Abstract

Taking advantage of microwave-assisted synthesis, efficient and expedite procedures for preparation of a library of fusaric acid and 39 analogues are reported. The fusaric acid analogues were tested in cell-based screening assays for inhibition of the las and rhl quorum sensing system in Pseudomonas aeruginosa and the lux quorum sensing system in Vibrio fischeri. Eight of the 40 compounds in the library including fusaric acid inhibited lux quorum sensing and one compound inhibited activity of the las quorum sensing system. To our delight, none of the compounds showed growth inhibitory effects in the tested concentration ranges.

Keywords: Fusaric acid; Microwave-assisted synthesis; Quorum sensing inhibitors.

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