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Synthesis and evaluation of new arylbenzo[b]thiophene and diarylthiophene derivatives as inhibitors of the NorA multidrug transporter of Staphylococcus aureus by Jérémie Fournier dit Chabert; Béatrice Marquez; Luc Neville; Lionel Joucla; Sylvie Broussous; Pascale Bouhours; Emilie David; Stéphane Pellet-Rostaing; Bernard Marquet; Nicole Moreau; Marc Lemaire is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Synthesis and evaluation of new arylbenzo[b]thiophene and diarylthiophene derivatives as inhibitors of the NorA multidrug transporter of Staphylococcus aureus about?
The synthesis based on palladium catalytic coupling of 38 new-arylated benzo[b]thiophenes or thiophenes is described in a few steps. We also report the direct arylation of the position 3 of the benzo[b]thiophenic structure, a 'one pot' 2,5-heterodiarylation of thiophenes as well as the synthesis of precursors of amino-acids with a 2-arylated benzo[b]thiophene core. These compounds were evaluated on bacteria strains: most of them did not exhibit any antibiotic activity but were found to selectively inhibit the NorA multidrug transporter of Staphylococcus aureus. As such, they restored the activity of the NorA substrates ciprofloxacin against a resistant S. aureus strain in which this efflux pump is over-expressed.
Who reads Synthesis and evaluation of new arylbenzo[b]thiophene and diarylthiophene derivatives as inhibitors of the NorA multidrug transporter of Staphylococcus aureus?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Jérémie Fournier dit Chabert; Béatrice Marquez; Luc Neville; Lionel Joucla; Sylvie Broussous; Pascale Bouhours; Emilie David; Stéphane Pellet-Rostaing; Bernard Marquet; Nicole Moreau; Marc Lemaire
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2007
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)