N-alkylated linear heptamethine polyenes as potent non-azole leads against Candida albicans fungal infections

Bioorg Chem. 2020 Sep:102:104070. doi: 10.1016/j.bioorg.2020.104070. Epub 2020 Jul 6.

Abstract

In this study, eighteen heptamethine dyes were synthesised and their antifungal activities were evaluated against three clinically relevant yeast species.. The eighteen dyes were placed within classes based on their core subunit i.e. 2,3,3-trimethylindolenine (5a-f), 1,1,2-trimethyl-1H-benzo[e]indole (6a-f), or 2-methylbenzothiazole (7a-f). The results presented herein imply that the three families of cyanine dyes, in particular compounds 5a-f, show high potential as selective scaffolds to treat C. albicans infections. This opens up the opportunity for further optimisation and investigation of this class compounds for potential antifungal treatment.

Keywords: Antifungal; Candida Albicans; Cyanine; Hepthamethine; Polyene.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / pharmacology
  • Antifungal Agents / therapeutic use*
  • Candida albicans / drug effects*
  • Humans
  • Molecular Structure
  • Polyenes / pharmacology
  • Polyenes / therapeutic use*

Substances

  • Antifungal Agents
  • Polyenes