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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.
Afiliação
  • Tung TT; Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen Ø, Denmark.
  • Jakobsen TH; Costerton Biofilm Center, Faculty of Health Sciences, Department of Immunology and Microbiology, Blegdamsvej 3B, 2200 Copenhagen, Denmark.
  • Dao TT; Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen Ø, Denmark; Department of Plant and Environmental Sciences, University of Copenhagen, Thorvaldsensvej 40, 1871 Frederiksberg C, Denmark.
  • Fuglsang AT; Department of Plant and Environmental Sciences, University of Copenhagen, Thorvaldsensvej 40, 1871 Frederiksberg C, Denmark.
  • Givskov M; Costerton Biofilm Center, Faculty of Health Sciences, Department of Immunology and Microbiology, Blegdamsvej 3B, 2200 Copenhagen, Denmark; Singapore Centre for Environmental Life Sciences Engineering (SCELSE), Nanyang Technological University, 637551, Singapore.
  • Christensen SB; Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen Ø, Denmark. Electronic address: soren.christensen@sund.ku.dk.
  • Nielsen J; Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen Ø, Denmark. Electronic address: john.nielsen@sund.ku.dk.
Eur J Med Chem ; 126: 1011-1020, 2017 Jan 27.
Article em En | MEDLINE | ID: mdl-28033578
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pseudomonas aeruginosa / Desenho de Fármacos / Ácido Fusárico / Percepção de Quorum Idioma: En Ano de publicação: 2017 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pseudomonas aeruginosa / Desenho de Fármacos / Ácido Fusárico / Percepção de Quorum Idioma: En Ano de publicação: 2017 Tipo de documento: Article