Amoebicidal effect of 5,5′‐[(4‐nitrophenyl)methylene]bis‐6‐hydroxy‐2‐mercapto‐3‐methyl‐4(3 H )‐pyrimidinone), a new drug against Entamoeba histolytica,Archiv der Pharmazie

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Amoebicidal effect of 5,5′‐[(4‐nitrophenyl)methylene]bis‐6‐hydroxy‐2‐mercapto‐3‐methyl‐4(3 H )‐pyrimidinone), a new drug against Entamoeba histolytica
Archiv der Pharmazie ( IF 4.3 ) Pub Date : 2020-10-05 , DOI: 10.1002/ardp.202000263
José L Vique-Sánchez ₁ , Albertana Jiménez-Pineda ₂ , Claudia G Benítez-Cardoza ₂

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Entamoeba histolytica is a cosmopolitan protozoan parasite that can produce infections in the intestine and some organs (liver, lungs, and brain), with worldwide prevalence. There are treatments against E. histolytica (antiparasitics), but as the drugs used in these treatments have presented some type of resistance and/or side effects, there are cases with complications of this disease. Therefore, it is necessary to develop new drugs aimed at a specific therapeutic target against this parasite. Here, we used the compound 5,5'-[(4-nitrophenyl)methylene]bis(6-hydroxy-2-mercapto-3-methyl-4(3H)-pyrimidinone) in the patenting process (called D4). D4 has a reported specific use against a glycolytic enzyme, the triosephosphate isomerase of Trichomonas vaginalis (TvTIM). We determined that D4 has an amoebicidal effect in in vitro cultures, with an IC50 value of 18.5 µM, and we proposed a specific site of interaction (Lys77, His110, Gln115, and Glu118) in the triosephosphate isomerase of E. histolytica (EhTIM). Furthermore, compound D4 has favorable experimental and theoretical toxicity results. Therefore, D4 should be further investigated as a potential drug against E. histolytica.

中文翻译：

5,5'-[(4-nitrophenyl)methylene]bis-6-hydroxy-2-mercapto-3-methyl-4(3H)-pyrimidinone)，一种抗溶组织内阿米巴新药的阿米巴虫作用

溶组织内阿米巴是一种全球性原生动物寄生虫，可在肠道和某些器官（肝、肺和脑）中产生感染，在世界范围内流行。有针对溶组织肠杆菌（抗寄生虫药）的治疗方法，但由于这些治疗中使用的药物存在某种类型的耐药性和/或副作用，因此有些病例会出现这种疾病的并发症。因此，有必要开发针对这种寄生虫的特定治疗靶点的新药。在这里，我们在专利申请过程中使用了化合物 5,5'-[(4-nitrophenyl)methylene]bis(6-hydroxy-2-mercapto-3-methyl-4(3H)-pyrimidinone)（称为 D4）。据报道，D4 具有针对糖酵解酶的特定用途，即阴道毛滴虫的丙糖磷酸异构酶 (TvTIM)。我们确定 D4 在体外培养中具有杀阿米巴作用，IC50 值为 18.5 µM，我们提出了溶组织大肠杆菌丙糖磷酸异构酶 (EhTIM) 中的特定相互作用位点（Lys77、His110、Gln115 和 Glu118）。此外，化合物D4具有良好的实验和理论毒性结果。因此，应进一步研究 D4 作为抗溶组织大肠杆菌的潜在药物。

更新日期：2020-10-05

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