European Journal of Medicinal Chemistry p. 1011 - 1020 (2017)
Update date:2022-08-04
Topics:
Tung, Truong Thanh
Jakobsen, Tim Holm
Dao, Trong Tuan
Fuglsang, Anja Thoe
Givskov, Michael
Christensen, S?ren Br?gger
Nielsen, John
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.
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