Synthesis, Characterization and Nanoformulation of Novel Sulfonamide-1,2,3-triazole Molecular Conjugates as Potent Antiparasitic Agents

Int J Mol Sci. 2022 Apr 11;23(8):4241. doi: 10.3390/ijms23084241.

Abstract

Toxoplasma gondii (T. gondii) is a highly prevalent parasite that has no gold standard treatment due to the poor action or the numerous side effects. Focused sulfonamide-1,2,3-triazole hybrids 3a-c were wisely designed and synthesized via copper catalyzed 1,3-dipolar cycloaddition approach between prop-2-yn-1-alcohol 1 and sulfa drug azides 2a-c. The newly synthesized click products were fully characterized using different spectroscopic experiments and were loaded onto chitosan nanoparticles to form novel nanoformulations for further anti-Toxoplasma investigation. The current study proved the anti-Toxoplasma effectiveness of all examined compounds in experimentally infected mice. Relative to sulfadiazine, the synthesized sulfonamide-1,2,3-triazole (3c) nanoformulae demonstrated the most promising result for toxoplasmosis treatment as it resulted in 100% survival, 100% parasite reduction along with the remarkable histopathological improvement in all the studied organs.

Keywords: 1,2,3-triazoles; Toxoplasma gondii; nanoformulation; sulfadiazine analogues.

MeSH terms

  • Animals
  • Antiparasitic Agents / pharmacology
  • Mice
  • Sulfonamides / pharmacology
  • Toxoplasma*
  • Toxoplasmosis*
  • Triazoles / chemistry

Substances

  • Antiparasitic Agents
  • Sulfonamides
  • Triazoles