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新型磺酰胺-1,2,3-三唑分子缀合物的合成、表征及纳米制剂作为有效的抗寄生虫药物。

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

机构信息

Department of Chemistry, College of Science, Taibah University, Al-Madinah Al-Munawarah 30002, Saudi Arabia.

Department of Medical Laboratory Technology, Faculty of Applied Health Sciences Technology, Pharos University in Alexandria, Alexandria 21321, Egypt.

出版信息

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

Abstract

() 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 were wisely designed and synthesized via copper catalyzed 1,3-dipolar cycloaddition approach between prop-2-yn-1-alcohol and sulfa drug azides . 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 () 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.

摘要

()是一种高流行的寄生虫,由于作用不佳或副作用众多,尚无金标准治疗方法。通过铜催化的丙炔-1-醇与磺胺药物叠氮化物之间的 1,3-偶极环加成反应,巧妙地设计并合成了靶向磺胺-1,2,3-三唑杂合体。新合成的点击产物使用不同的光谱实验进行了充分的表征,并负载到壳聚糖纳米颗粒上,以形成用于进一步抗弓形虫研究的新型纳米制剂。本研究证明了所有检查化合物在实验感染小鼠中的抗弓形虫作用。与磺胺嘧啶相比,合成的磺胺-1,2,3-三唑()纳米制剂在弓形虫病治疗方面显示出最有希望的结果,因为它导致 100%的存活率,100%的寄生虫减少,以及所有研究器官的显著组织病理学改善。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5d94/9025934/2786ef54f593/ijms-23-04241-g001.jpg

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