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Title
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In vitro evaluation of arylsubstituted imidazoles derivatives as antiprotozoal agents and docking studies on sterol 14-demethylase (CYP51) from Trypanosoma cruzi, Leishmania infantum, and Trypanosoma brucei
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Author
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Abstract
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| There is an urgent need to discover and develop new drugs to combat parasitic diseases as Chagas disease (Trypanosoma cruzi), sleeping sickness (Trypanosoma brucei), and leishmaniasis (Leishmania ssp.). These diseases are considered among the 13 most unattended diseases worldwide according to the WHO. In the present work, the synthesis of 14 arylsubstituted imidazoles and its molecular docking onto sterol 14-demethylase (CYP51) was executed. In addition, the compounds, antiprotozoal activity against T. brucei, T. cruzi, Trypanosoma brucei rhodesiense, and Leishmania infantum was evaluated. In vitro antiparasitic results of the arylsubstituted imidazoles against T. brucei, T. cruzi, T.b. rhodesiense, and L. infantum indicated that all samples from arylsubstituted imidazole compounds presented interesting antiparasitic activity to various extent. The ligands 5a, 5c, 5e, 5f, 5g, 5i, and 5j exhibited strong activity against T. brucei, T. cruzi, T.b. rhodesiense, and L. infantum with IC50 values ranging from 0.86 to 10.23M. Most samples were cytotoxic against MRC-5 cell lines (1.12 |
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Language
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English
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Source (journal)
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Parasitology research / Deutsche Gesellschaft für Parasitologie. - Berlin, 1987, currens
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Publication
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Berlin
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Springer
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2019
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ISSN
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0932-0113
[print]
1432-1955
[online]
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DOI
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10.1007/S00436-019-06206-Z
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Volume/pages
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118
:5
(2019)
, p. 1533-1548
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ISI
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000465507800020
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Pubmed ID
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30903349
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Full text (Publisher's DOI)
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Full text (publisher's version - intranet only)
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