Title: Identification And Characterization Of 4-[4-(3-Phenyl-2-propen-1-yl)-1-Piperazinyl]-5H-Pyrimido[5,4-B]Indole Derivatives As Salmonella Biofilm Inhibitors
Other Titles: Identification of new Salmonella biofilm inhibitors
Authors: Robijns, Stijn ×
De Pauw, B.
Loosen, B.
Marchand, A.
Chaltin, P.
De Keersmaecker, Sigrid
Vanderleyden, Jos #
Issue Date: 8-May-2012
Publisher: Elsevier Science Publishers, B.V. on behalf of the Federation of European Microbiological Societies
Series Title: FEMS Immunology and Medical Microbiology vol:doi: 10.1111/j.1574-695X.2012.00973.x.
Abstract: A screening of a small-molecule library was conducted, in search of Salmonella biofilm inhibitors active in a broad temperature range, both in prevention and eradication of biofilms. Moreover, the inhibitors were selected not to influence the planktonic growth of Salmonella in order to diminish the selective pressure and to prevent or slow down resistance development. Out of the 20,014 compounds screened at 16 and 37 °C, 140 hits were identified. After characterization of the most promising hits at a broader set of temperatures (16, 25, 30 and 37 °C), we identified 7-methoxy-4-[4-(3-phenyl-2-propen-1-yl)-1-piperazinyl]-5H-pyrimido[5,4-b]indole as an interesting preventive anti-biofilm compound. A first structure-activity relationship of this compound was delineated, revealing 8-fluoro-4-[4-(3-phenyl-2-propen-1-yl)-1-piperazinyl]-5H-pyrimido[5,4-b]indole as a promising analogue in the prevention of Salmonella biofilms.
ISSN: 0928-8244
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Centre of Microbial and Plant Genetics
× corresponding author
# (joint) last author

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