Anti-protozoal and anti-fungal evaluation of 3,5-disubstituted 1,2-dioxolanes

Bioorg Med Chem Lett. 2021 Sep 1:47:128196. doi: 10.1016/j.bmcl.2021.128196. Epub 2021 Jun 8.

Abstract

Endoperoxides are a class of compounds, which is well-known for their antimalarial properties, but few reports exist about 3,5-disubstituted 1,2-dioxolanes. After having designed a new synthetic route for the preparation of these substances, they were evaluated against 4 different agents of infectious diseases, protozoa (Plasmodium and Leishmania) and Fungi (Candida and Aspergillus). Whereas moderate antifungal activity was found for our products, potent antimalarial and antileishmanial activities were observed for a few compounds. The nature of the substituents linked to the endoperoxide ring seems to play an important role in the bioactivities.

Keywords: 1,2-Dioxolane; Antifungal; Antileishmanial; Antimalarial; Endoperoxide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Antiprotozoal Agents / chemical synthesis
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Aspergillus / drug effects
  • Candida / drug effects
  • Dioxolanes / chemical synthesis
  • Dioxolanes / chemistry
  • Dioxolanes / pharmacology*
  • Dose-Response Relationship, Drug
  • Leishmania / drug effects
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Plasmodium / drug effects
  • Structure-Activity Relationship

Substances

  • Antifungal Agents
  • Antiprotozoal Agents
  • Dioxolanes