Esters of quinoxaline-7-carboxylate-1,4-di-N-oxide as Trichomonas vaginalis triosephosphate isomerase inhibitors
| Autor: | Rosa Moo-Puc, Claudia G. Benítez-Cardoza, José Luis Vique-Sánchez, Juan Carlos Villalobos-Rocha, Antonio Monge, Gildardo Rivera, Alma D Paz-González, Isidro Palos |
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| Rok vydání: | 2020 |
| Předmět: |
Pharmacology
0303 health sciences 4-di-n-oxide Stereochemistry Oxide Pharmaceutical Science General Medicine medicine.disease_cause triosephosphate isomerase inhibitor Triosephosphate isomerase 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Quinoxaline chemistry 030220 oncology & carcinogenesis quinoxaline 1 medicine trichomoniasis Trichomonas vaginalis quinoxaline 1 4-di-N-oxide Carboxylate HD9665-9675 Pharmaceutical industry 030304 developmental biology |
| Zdroj: | Acta Pharmaceutica, Vol 71, Iss 3, Pp 485-495 (2021) Acta Pharmaceutica Volume 71 Issue 3 |
| ISSN: | 1846-9558 1330-0075 |
| Popis: | 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 in in vitro assays as novel trichomonicidal agents. Additionally, an in vitro enzyme assay and molecular docking analysis against triosephosphate isomerase of Trichomonas vaginalis to confirm their mechanism of action were performed. Ethyl (compound 12) and n-propyl (compound 37) esters of quinoxaline-7-carboxy-late-1,4-di-N-oxide derivatives showed trichomonicidal activity comparable to nitazoxanide, whereas five methyl (compounds 5, 15, 19, 20 and 22), four isopropyl (compounds 28, 29, 30 and 34), three ethyl (compounds 4, 13 and 23) and one npropyl (compound 35) ester derivatives displayed activity comparable to albendazole. Compounds 6 and 20 decreased 100 % of the enzyme activity of recombinant protein triosephosphate isomerase. |
| Databáze: | OpenAIRE |
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