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

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...

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Main Authors: Tung, Truong Thanh, Jakobsen, Tim Holm, Dao, Trong Tuan, Fuglsang, Anja Thoe, Givskov, Michael, Christensen, Søren Brøgger, Nielsen, John
Other Authors: Singapore Centre for Environmental Life Sciences Engineering
Format: Article
Language:English
Published: 2017
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Online Access:https://hdl.handle.net/10356/83479
http://hdl.handle.net/10220/42594
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Institution: Nanyang Technological University
Language: English
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spelling sg-ntu-dr.10356-834792020-09-21T11:34:40Z Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors Tung, Truong Thanh Jakobsen, Tim Holm Dao, Trong Tuan Fuglsang, Anja Thoe Givskov, Michael Christensen, Søren Brøgger Nielsen, John Singapore Centre for Environmental Life Sciences Engineering Quorum sensing inhibitors Fusaric acid 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. Accepted version 2017-06-06T08:44:56Z 2019-12-06T15:23:53Z 2017-06-06T08:44:56Z 2019-12-06T15:23:53Z 2016 Journal Article Tung, T. T., Jakobsen, T. H., Dao, T. T., Fuglsang, A. T., Givskov, M., Christensen, S. B., et al. (2017). Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors. European Journal of Medicinal Chemistry, 126, 1011-1020. 0223-5234 https://hdl.handle.net/10356/83479 http://hdl.handle.net/10220/42594 10.1016/j.ejmech.2016.11.044 en European Journal of Medicinal Chemistry © 2016 Elsevier. This is the author created version of a work that has been peer reviewed and accepted for publication by European Journal of Medicinal Chemistry, Elsevier. It incorporates referee’s comments but changes resulting from the publishing process, such as copyediting, structural formatting, may not be reflected in this document. The published version is available at: [http://dx.doi.org/10.1016/j.ejmech.2016.11.044]. 46 p. application/pdf
institution Nanyang Technological University
building NTU Library
country Singapore
collection DR-NTU
language English
topic Quorum sensing inhibitors
Fusaric acid
spellingShingle Quorum sensing inhibitors
Fusaric acid
Tung, Truong Thanh
Jakobsen, Tim Holm
Dao, Trong Tuan
Fuglsang, Anja Thoe
Givskov, Michael
Christensen, Søren Brøgger
Nielsen, John
Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors
description 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.
author2 Singapore Centre for Environmental Life Sciences Engineering
author_facet Singapore Centre for Environmental Life Sciences Engineering
Tung, Truong Thanh
Jakobsen, Tim Holm
Dao, Trong Tuan
Fuglsang, Anja Thoe
Givskov, Michael
Christensen, Søren Brøgger
Nielsen, John
format Article
author Tung, Truong Thanh
Jakobsen, Tim Holm
Dao, Trong Tuan
Fuglsang, Anja Thoe
Givskov, Michael
Christensen, Søren Brøgger
Nielsen, John
author_sort Tung, Truong Thanh
title Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors
title_short Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors
title_full Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors
title_fullStr Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors
title_full_unstemmed Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors
title_sort fusaric acid and analogues as gram-negative bacterial quorum sensing inhibitors
publishDate 2017
url https://hdl.handle.net/10356/83479
http://hdl.handle.net/10220/42594
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