文章基本信息

标题：Esters of quinoxaline-7-carboxylate-1,4-di- N-oxide as Trichomonas vaginalis triosephosphate isomerase inhibitors
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作者：Isidro Palos ; Rosa Moo-Puc ; José Luis Vique-Sánchez 等
期刊名称：Acta Pharmaceutica
电子版ISSN：1846-9558
出版年度：2021
卷号：71
期号：3
页码：485-495
DOI：10.2478/acph-2021-0032
语种：English
出版社：Sciendo
摘要：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-N-oxide (EQX-NO) were evaluated inin vitroassays as novel trichomonicidal agents. Additionally, anin vitroenzyme assay and molecular docking analysis against triosephosphate isomerase ofTrichomonas vaginalisto confirm their mechanism of action were performed. Ethyl (compound12) andn-propyl (compound37) esters of quinoxaline-7-carboxy-late-1,4-di-N-oxide derivatives showed trichomonicidal activity comparable to nitazoxanide, whereas five methyl (compounds5,15,19,20and22), four isopropyl (compounds28,29,30and34), three ethyl (compounds4,13and23) and onenpropyl (compound35) ester derivatives displayed activity comparable to albendazole. Compounds6and20decreased 100 % of the enzyme activity of recombinant protein triosephosphate isomerase.