Méndez-Arriaga José M, Rubio-Mirallas Erika, Quirós Miguel, Sánchez-Moreno Manuel
Departamento de Biología y Geología, Física y Química Inorganica, Universidad Rey Juan Carlos, c/Tulipán s/n 28933, Móstoles, Madrid, Spain.
Departamento de Parasitología, Universidad de Granada, Avda. Fuentenueva s/n, 18071 Granada, Spain.
Med Chem. 2022;18(4):444-451. doi: 10.2174/1573406417666210812162500.
The World Health Organization catalogues illnesses such as Chagas disease as neglected diseases, due to the low investment in new drugs to fight them. The search for novel and non-side effects anti-parasitic compounds is one of the urgent needs of the Third World. The use of triazolopyrimidines and their metal complexes have demonstrated hopeful results in this field.
This work studies the antiparasitic efficacy against Trypanosoma cruzi strains of a series of zinc triazolopyrimidine complexes.
A series of Zn complexes has been synthesized by the reaction between the triazolopyrimidine derivatives 7-amino-1,2,4-triazolo[1,5-a]pyrimidine (7atp) and 5,7-dimethyl-1,2,4-triazolo[1,5- a]pyrimidine (dmtp) with Zn(SO) · 7HO, ZnCl, and Zn(NO) · 6HO salts. The complexes have been analyzed by spectroscopic and thermal assays and X-ray diffraction methods have been used to dilucidate the crystalline structure of one of them. The antiparasitic efficacy was tested in vitro against Trypanosoma cruzi to compare the trypanocidal effect of different ligands and counteranions to fight Chagas disease.
The efficacy of these compounds against Trypanosoma cruzi has also been tested to compare the influence of different ligands and counteranions on the trypanocidal effect against Chagas disease.
Antiproliferative tests corroborate the synergistic trypanocidal effect of the triazolopyrimidine coordination complexes.
世界卫生组织将恰加斯病等疾病列为被忽视的疾病，原因是对抗这些疾病的新药研发投入较低。寻找新型且无副作用的抗寄生虫化合物是第三世界的迫切需求之一。三唑并嘧啶及其金属配合物的应用在该领域已显示出令人期待的结果。
本研究旨在考察一系列三唑并嘧啶锌配合物对克氏锥虫菌株的抗寄生虫效果。
通过三唑并嘧啶衍生物7-氨基-1,2,4-三唑并[1,5-a]嘧啶（7atp）和5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶（dmtp）与硫酸锌·7水合物、氯化锌和硝酸锌·6水合物盐反应合成了一系列锌配合物。通过光谱和热分析对配合物进行了分析，并采用X射线衍射方法阐明了其中一种配合物的晶体结构。在体外对克氏锥虫进行抗寄生虫效果测试，以比较不同配体和抗衡阴离子对抗恰加斯病的杀锥虫效果。
还测试了这些化合物对克氏锥虫的效果，以比较不同配体和抗衡阴离子对恰加斯病杀锥虫效果的影响。
抗增殖试验证实了三唑并嘧啶配位配合物具有协同杀锥虫作用。
