Anticandidal formyl phloroglucinol meroterpenoids: Biomimetic synthesis and in vitro evaluation

Bioorg Chem. 2020 Nov:104:104248. doi: 10.1016/j.bioorg.2020.104248. Epub 2020 Sep 1.

Abstract

Inspired by the diversity-oriented synthesis, some novel formyl phloroglucinol meroterpenoids were synthesized via biomimetic synthesis using essential oils. Eight of them were demonstrated with good in vitro fungicidal activity against Candida albicans and C. glabrata. Compound c2 showed the best anticandidal ability that was powerfully comparable to fluconazole when testing against several strains in vitro. The antibiofilm activity was also found for the c2 treating group which was evidenced to block the hyphal elongation and filamentation of C. albicans. Therefore, compound c2 is a promising candidate for further antifungal-based structure modification.

Keywords: Antibiofilm activity; Anticandidal activity; Essential oil; Formyl phloroglucinol meroterpenoids.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Biomimetic Materials / chemical synthesis
  • Biomimetic Materials / chemistry
  • Biomimetic Materials / pharmacology*
  • Candida / drug effects*
  • Dose-Response Relationship, Drug
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Phloroglucinol / chemical synthesis
  • Phloroglucinol / chemistry
  • Phloroglucinol / pharmacology*
  • Structure-Activity Relationship
  • Terpenes / chemical synthesis
  • Terpenes / chemistry
  • Terpenes / pharmacology*

Substances

  • Antifungal Agents
  • Terpenes
  • Phloroglucinol