Antifungal evaluation of quinoline-chalcone derivatives combined with FLC against drug-resistant Candida albicans

Bioorg Med Chem Lett. 2023 Apr 15:86:129242. doi: 10.1016/j.bmcl.2023.129242. Epub 2023 Mar 15.

Abstract

With the widespread clinical use of FLC, the FLC-resistant C. albicans greatly increases the difficulty of treatment, and drug combination becomes an important method to treat C. albicans infection. In this work, we have prepared a series of quinoline-chalcone derivatives in good yields, and in vitro antifungal activity against C. albicans were evaluated. The results indicated that most title compounds combined with FLC showed good antifungal activity against drug-resistant C. albicans. Further mechanism researches demonstrated that 6a and 6c combined with FLC could significantly inhibited growth and biofilm formation of C. albicans, induce ROS accumulation, impair the mitochondrial membrane, and decrease intracellular ATP concentrations.

Keywords: Antifungal activity; Drug-resistant Candida albicans; Mechanistic study; Quinoline-chalcone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents* / pharmacology
  • Candida albicans
  • Chalcones* / pharmacology
  • Drug Resistance, Fungal
  • Drug Synergism
  • Fluconazole / pharmacology
  • Microbial Sensitivity Tests

Substances

  • Antifungal Agents
  • Fluconazole
  • Chalcones