Department of Clinical and Toxicological Analysis, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo-SP 05508-000, Brazil.
Fundação Centro Universitário Estadual da Zona Oeste, Unidade de Farmácia, Rio de Janeiro-RJ 23070-200, Brazil.
Biomolecules. 2020 Aug 18;10(8):1197. doi: 10.3390/biom10081197.
The search for new compounds with antimalarial activity is urgent, as resistance to ones in the classical drug, has already been described in more than one continent. Compounds derived from 1,2,3-triazoles are effective against parasites and bacteria. Here, we evaluated the potential antimalarial activity against the human malaria parasite in a culture of fifty-four triazole compounds derived from 1-and 2-1,2,3-triazole. We identified thirty-one compounds with potential antimalarial activity at concentrations in the micromolar order (µM) and IC values ranging from 2.80 µM () to 29.27 µM (). Then, we selected some of these compounds to perform the same tests on the PfSR25- strain (knockout for G-protein coupled receptor-like, SR25). Our experiences with the PfSR25- strain showed that both compounds with higher antimalarial activity for the 3D7 strain and those with less activity resulted in lower IC values for the knockout strain. The cytotoxicity of the compounds was evaluated in human renal embryonic cells (HEK 293), using MTT assays. This demonstrated that the compounds with the highest activity (, , , , , ), showed no toxicity at the tested concentrations.
寻找具有抗疟活性的新化合物是当务之急，因为在一个以上的大陆已经描述了对经典药物的耐药性。源自 1,2,3-三唑的化合物对寄生虫和细菌有效。在这里，我们评估了 54 种源自 1-和 2-1,2,3-三唑的三唑化合物对人类疟疾寄生虫 的潜在抗疟活性。我们发现 31 种化合物在微摩尔浓度下具有潜在的抗疟活性（µM），IC 值范围从 2.80 µM () 到 29.27 µM ()。然后，我们选择了其中一些化合物对 PfSR25-株（G 蛋白偶联受体样，SR25 的基因敲除）进行相同的测试。我们在 PfSR25-株上的经验表明，对于 3D7 株具有更高抗疟活性的两种化合物和活性较低的化合物，对于敲除株，IC 值均较低。通过 MTT 测定法评估了化合物在人肾胚胎细胞（HEK 293）中的细胞毒性。这表明，活性最高的化合物（，，，，，）在测试浓度下没有毒性。
