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

Faizah S. Aljohani, Nadjet Rezki, Mohamed Reda Aouad, Bassma H. Elwakil, Mohamed Hagar, Eman Sheta, Nermine Mogahed Fawzy Hussein Mogahed, Sanaa K. Bardaweel, Nancy Abd‐elkader Hagras

2022International Journal of Molecular Sciences28 citationsDOIOpen Access PDF

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.

Topics & Concepts

SulfadiazineToxoplasma gondiiSulfonamideAntiparasiticClick chemistryTriazoleChemistryCombinatorial chemistryAntiparasitic agentConjugatePharmacologyStereochemistryBiologyMedicineAntibioticsAntibodyBiochemistryOrganic chemistryImmunologyPathologyMathematicsMathematical analysisClick Chemistry and ApplicationsSynthesis and Characterization of Heterocyclic CompoundsSynthesis and Biological Evaluation
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