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

TY - JOUR

T1 - Fusaric acid and analogues as gram-negative bacterial quorum sensing inhibitors

AU - Thanh Tung, Truong

AU - Jakobsen, Tim Holm

AU - Dao, Trong Tuan

AU - Fuglsang, Anja Thoe

AU - Givskov, Michael

AU - Christensen, Søren Brøgger

AU - Nielsen, John

PY - 2017

Y1 - 2017

N2 - 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.

AB - 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.

U2 - 10.1016/j.ejmech.2016.11.044

DO - 10.1016/j.ejmech.2016.11.044

M3 - Journal article

C2 - 28033578

SN - 0223-5234

VL - 126

SP - 1011

EP - 1020

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -