Esters of quinoxaline-7-carboxylate-1,4-di--oxide as triosephosphate isomerase inhibitors.

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.