Palos Isidro, Moo-Puc Rosa, Vique-Sánchez José Luis, Benítez-Cardoza Claudia G, Monge Antonio, Villalobos-Rocha Juan Carlos, Paz-Gonzalez Alma D, Rivera Gildardo
Unidad Académica Multidisciplinaria, Reynosa-Rodhe, Universidad Autónoma de Tamaulipas, 88779 Reynosa, México.
Unidad de Investigación Médica Yucatán, Unidad Médica de Alta Especialidad, Centro Médico Ignacio García Téllez, Instituto Mexicano del Seguro Social Col. Industrial, 97150 Mérida, México.
Acta Pharm. 2020 Dec 31;71(3):485-495. doi: 10.2478/acph-2021-0032. Print 2021 Sep 1.
Trichomoniasis is a public health problem worldwide. Trichomoniasis treatment consists of the use of nitroimidazole derivatives; however, therapeutic ineffectiveness occurs in 5 to 20 % of the cases. Therefore, it is essential to propose new pharmacological agents against this disease. In this work, esters of quinoxaline-7-carboxylate-1,4-di--oxide (EQX-O) were evaluated in assays as novel trichomonicidal agents. Additionally, an enzyme assay and molecular docking analysis against triosephosphate isomerase of to confirm their mechanism of action were performed. Ethyl (compound ) and -propyl (compound ) esters of quinoxaline-7-carboxy-late-1,4-di--oxide derivatives showed trichomonicidal activity comparable to nitazoxanide, whereas five methyl (compounds , , , and ), four isopropyl (compounds , , and ), three ethyl (compounds , and ) and one propyl (compound ) ester derivatives displayed activity comparable to albendazole. Compounds and decreased 100 % of the enzyme activity of recombinant protein triosephosphate isomerase.
滴虫病是一个全球性的公共卫生问题。滴虫病的治疗包括使用硝基咪唑衍生物；然而，5%至20%的病例会出现治疗无效的情况。因此，提出针对这种疾病的新药理学制剂至关重要。在这项工作中，喹喔啉 - 7 - 羧酸 - 1,4 - 二氧化物（EQX - O）的酯类作为新型杀滴虫剂在试验中进行了评估。此外，还进行了针对磷酸丙糖异构酶的酶测定和分子对接分析以确认其作用机制。喹喔啉 - 7 - 羧酸 - 1,4 - 二氧化物衍生物的乙酯（化合物 ）和 - 丙酯（化合物 ）表现出与硝唑尼特相当的杀滴虫活性，而五种甲酯（化合物 、 、 、 和 ）、四种异丙酯（化合物 、 、 和 ）、三种乙酯（化合物 、 和 ）以及一种丙酯（化合物 ）衍生物表现出与阿苯达唑相当的活性。化合物 和 使重组蛋白磷酸丙糖异构酶的酶活性降低了100%。
