Open AccessIdentification and characterization of 4‐[4‐(3‐phenyl‐2‐propen‐1‐yl)‐1‐piperazinyl]‐ 5 H ‐pyrimido[5,4‐b]indole derivatives as S almonella biofilm inhibitors
Author(s) -
Robijns Stijn Chris Arnold,
Pauw Bart,
Loosen Bram,
Marchand Arnaud,
Chaltin Patrick,
Keersmaecker Sigrid C. J.,
Vanderleyden Jos,
Steenackers Hans P. L.
Publication year - 2012
Publication title -
fems immunology & medical microbiology
Language(s) - English
Resource type - Journals
eISSN - 1574-695X
pISSN - 0928-8244
DOI - 10.1111/j.1574-695x.2012.00973.x
Subject(s) - indole test , salmonella , microbiology and biotechnology , biofilm , biology , identification (biology) , stereochemistry , bacteria , chemistry , botany , genetics
A screening of a small‐molecule library was conducted, in search of S almonella biofilm inhibitors active in a broad temperature range, both in prevention and in eradication of biofilms. Moreover, the inhibitors were selected not to influence the planktonic growth of S almonella 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]‐ 5 H ‐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]‐ 5 H ‐pyrimido[5,4‐b]indole as a promising analogue in the prevention of S almonella biofilms.