Biological Insights of Fluoroaryl-2,2′-Bichalcophene Compounds on Multi-Drug Resistant <i>Staphylococcus aureus</i>

• Main Authors: Sally Elmogy, Mohamed A. Ismail, Rabeay Y. A. Hassan, Ahmed Noureldeen, Hadeer Darwish, Eman Fayad, Fahmy Elsaid, Ashraf Elsayed
• Format: Article
• Language: English
• Published: MDPI AG 2021-12-01
• Series: Molecules
• Subjects: bichalcophene derivatives; <i>S. aureus</i>; antibacterial activity; anti-biofilm agents; biosensors
• Online Access: https://www.mdpi.com/1420-3049/26/1/139

Resistance of bacteria to multiple antibiotics is a significant health problem; hence, to continually respond to this challenge, different antibacterial agents must be constantly discovered. In this work, fluoroaryl-2,2′-bichalcophene derivatives were chemically synthesized and their biological activities were evaluated against <i>Staphylococcus aureus</i> (<i>S. aureus</i>). The impact of the investigated bichalcophene derivatives was studied on the ultrastructural level via scanning electron microscopy (SEM), molecular level via sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) method and on the biofilm inhibition via the electrochemical biosensors. Arylbichalcophenes’ antibacterial activity against <i>S. aureus</i> was affected by the presence and location of fluorine atoms. The fluorobithiophene derivative <b>MA-1156</b> displayed the best minimum inhibitory concentration (MIC) value of 16 µM among the tested fluoroarylbichalcophenes. Over a period of seven days, <i>S. aureus</i> did not develop any resistance against the tested fluoroarylbichalcophenes at higher concentrations. The impact of fluoroarylbichalcophenes was strong on <i>S. aureus</i> protein pattern showing high degrees of polymorphism. SEM micrographs of <i>S. aureus</i> cells treated with fluoroarylbichalcophenes displayed smaller cell-sizes, fewer numbers, arranged in a linear form and some of them were damaged when compared to the untreated cells. The bioelectrochemical measurements demonstrated the strong sensitivity of <i>S. aureus</i> cells to the tested fluoroarylbichalcophenes and an antibiofilm agent. Eventually, these fluoroarylbichalcophene compounds especially the <b>MA-1156</b> could be recommended as effective antibacterial agents.