Esters of quinoxaline-7-carboxylate-1,4-di- N -oxide as Trichomonas vaginalis triosephosphate isomerase inhibitors
Abstract
Abstract
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-
N
O) 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
n
propyl (compound
35
) ester derivatives displayed activity comparable to albendazole. Compounds
6
and
20
decreased 100 % of the enzyme activity of recombinant protein triosephosphate isomerase.
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