New Chalcone–Triazole Hybrids with Promising Antimicrobial Activity in Multidrug Resistance Strains

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Abstract
Resistance to antibiotics is an emerging problem worldwide, which leads to an increase in morbidity and mortality rates. Several mechanisms are attributed to bacterial resistance, overexpression of efflux pumps being one of the most prominent. As an attempt to develop new effective antimicrobial drugs, which could be able to act against resistant bacterial strains and considering the antimicrobial potential of flavonoids and triazolyl flavonoid derivatives, in particular chalcones, a small library of chalcone derivatives was synthesized and evaluated for its potential to act as antimicrobials and/or adjuvants in combination with antibiotics towards resistant bacteria. Although only compound 7 was able to act as antibacterial, compounds 1, 2, 4, 5, 7, and 9 revealed to be able to potentiate the activity of antibiotics in resistant bacteria. Moreover, five compounds (3, 5–8) demonstrated to be effective inhibitors of efflux pumps in Salmonella enterica serovar Typhimurium SL1344, and four compounds (1, 3, 7, and 10) showed higher ability than reserpine to inhibit biofilm formation of resistant Staphylococcus aureus 272123. Together, our results showed the potential of these compounds regarding reversion of bacterial resistance.
Funding Information
  • FCT-Foundation for Science and Technology (UIDB/04423/2020, UIDP/04423/2020, PTDC/SAU-PUB/28736/2017, EXPL/CTA-AMB/0810/2021, PTDC/CTA-AMB/0853/2021, CHIRALBIOACTIVE-PI-3RL-IINFACTS-2019, CHIRALSINTESE_APSFCT_IINFACTS _2021, SFRH/BD/147207/2019, SFRH/BD/144681/2019, BO/00158/22/5)
  • IINFACTS (UIDB/04423/2020, UIDP/04423/2020, PTDC/SAU-PUB/28736/2017, EXPL/CTA-AMB/0810/2021, PTDC/CTA-AMB/0853/2021, CHIRALBIOACTIVE-PI-3RL-IINFACTS-2019, CHIRALSINTESE_APSFCT_IINFACTS _2021, SFRH/BD/147207/2019, SFRH/BD/144681/2019, BO/00158/22/5)
  • FCT (UIDB/04423/2020, UIDP/04423/2020, PTDC/SAU-PUB/28736/2017, EXPL/CTA-AMB/0810/2021, PTDC/CTA-AMB/0853/2021, CHIRALBIOACTIVE-PI-3RL-IINFACTS-2019, CHIRALSINTESE_APSFCT_IINFACTS _2021, SFRH/BD/147207/2019, SFRH/BD/144681/2019, BO/00158/22/5)
  • Hungarian Academy of Sciences (UIDB/04423/2020, UIDP/04423/2020, PTDC/SAU-PUB/28736/2017, EXPL/CTA-AMB/0810/2021, PTDC/CTA-AMB/0853/2021, CHIRALBIOACTIVE-PI-3RL-IINFACTS-2019, CHIRALSINTESE_APSFCT_IINFACTS _2021, SFRH/BD/147207/2019, SFRH/BD/144681/2019, BO/00158/22/5)

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