期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 22, 期 2, 页码 227-233出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756360601051233
关键词
Trypanosoma cruzi; (alpha-hydroxyacid dehydrogenase-isozyme II inhibition; ethyl N-allyl oxamate; ethyl N-propyl oxamate; (alpha-hydroxyacid dehydrogenase (HADH)
The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters of N-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes ( in vitro) and murine trypanosomiasis ( in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact epimastigotes and therefore we were not able to detect any trypanocidal effect with these oxamates. Whereas the ethyl esters (Et-NAOx and Et-NPOx), acting as prodrugs, exhibited in vitro and in vivo trypanocidal activity on the five tested T. cruzi strains. On the contrary, when Nifurtimox and Benznidazole used as reference drugs were tested, we found that only three of the five tested T. cruzi strains were affected, whereas the other two strains, Miguz and Compostela, were resistant to the in vitro and in vivo trypanocidal activity of these compounds.
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