1. Design, Synthesis, and Evaluation of Alkyl-Quinoxalin-2(1H)-One Derivatives as Anti-Quorum Sensing Molecules, Inhibiting Biofilm Formation in Aeromonas caviae Sch3
- Author
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René Blöcher, Graciela Castro-Escarpulli, Everardo Curiel-Quesada, Alicia Reyes-Arellano, and Ariel Rodarte Ramírez
- Subjects
0301 basic medicine ,Aeromonas caviae ,030106 microbiology ,Pharmaceutical Science ,biofilm ,Analytical Chemistry ,Microbiology ,lcsh:QD241-441 ,03 medical and health sciences ,Antibiotic resistance ,lcsh:Organic chemistry ,Drug Discovery ,bioisosteres ,Physical and Theoretical Chemistry ,anti-quorum sensing ,Alkyl ,chemistry.chemical_classification ,biology ,Chemistry ,Drug discovery ,Organic Chemistry ,Biofilm ,Grignard reaction ,biology.organism_classification ,Small molecule ,Quorum sensing ,quinoxalin-2(1H)-one ,030104 developmental biology ,Chemistry (miscellaneous) ,Molecular Medicine ,Bacteria - Abstract
With the increasing antibiotic resistance of bacterial strains, alternative methods for infection control are in high demand. Quorum sensing (QS) is the bacterial communication system based on small molecules. QS is enables bacterial biofilm formation and pathogenic development. The interruption of QS has become a target for drug discovery, but remains in the early experimental phase. In this study, we synthesized a set of six compounds based on a scaffold (alkyl-quinoxalin-2(1H)-one), new in the anti-QS of Gram-negative bacteria Aeromonas caviae Sch3. By quantifying biofilm formation, we were able to monitor the effect of these compounds from concentrations of 1 to 100 µM. Significant reduction in biofilm formation was achieved by 3-hexylylquinoxalin-2(1H)-one (11), 3-hexylylquinoxalin-2(1H)-one-6-carboxylic acid (12), and 3-heptylylquinoxalin-2(1H)-one-6-carboxylic acid (14), ranging from 11% to 59% inhibition of the biofilm. This pilot study contributes to the development of anti-QS compounds to overcome the clinical challenge of resistant bacteria strains.
- Published
- 2018