Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors

Molecules. 2020 Jan 15;25(2):345. doi: 10.3390/molecules25020345.

Abstract

Styrylquinolines are heterocyclic compounds that are known for their antifungal and antimicrobial activity. Metal complexation through hydroxyl groups has been claimed to be a plausible mechanism of action for these types of compounds. A series of novel structures with protected hydroxyl groups have been designed and synthesized to verify the literature data. Their antifungal activity against wild-type Candida albicans strain and mutants with silenced efflux pumps activity has been determined. Combinations with fluconazole revealed synergistic interactions that were dependent on the substitution pattern. These results open a new route for designing active antifungal agents on a styrylquinoline scaffold.

Keywords: ABC transporters; Candida albicans; Cdr1p; styrylquinolines.

MeSH terms

  • ATP-Binding Cassette Transporters / antagonists & inhibitors*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Candida albicans / drug effects*
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Rhodamines / metabolism

Substances

  • ATP-Binding Cassette Transporters
  • Antifungal Agents
  • Quinolines
  • Rhodamines
  • styrylquinoline
  • rhodamine 6G