Source:http://linkedlifedata.com/resource/pubmed/id/19616875
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
11
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pubmed:dateCreated |
2009-10-9
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pubmed:abstractText |
Exploring the influence of different substitution patterns of 2H-benzimidazole 1,3-dioxide derivatives (BzNO) we prepared fifteen new derivatives. Initially the BzNO were tested against Trypanosoma cruzi Tulahuen 2 strain epimastigote form rendering very potent anti-T. cruzi agents. Moreover, the BzNO were able to inhibit the growth of virulent and resistant to Benznidazole strains (CL Brener clone, Colombiana, and Y strains) and to Leishmania braziliensis. Interestingly, BzNO exhibited very high selectivity index and particularly the spiro-BzNO 13 provokes an important diminution of amastigotes in Vero cells. Besides, it was found a diminution of acetate and glycine as excreted metabolites but without increase of parasite glucose uptake indicating that the glycosome is probably not involucrate in the 2H-benzimidazole 1,3-dioxides mechanism of action.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Benzimidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Glucose,
http://linkedlifedata.com/resource/pubmed/chemical/Oxidoreductases,
http://linkedlifedata.com/resource/pubmed/chemical/Trypanocidal Agents,
http://linkedlifedata.com/resource/pubmed/chemical/benzimidazole
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1768-3254
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4426-33
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pubmed:meshHeading |
pubmed-meshheading:19616875-Animals,
pubmed-meshheading:19616875-Benzimidazoles,
pubmed-meshheading:19616875-Cell Line,
pubmed-meshheading:19616875-Cell Survival,
pubmed-meshheading:19616875-Chagas Disease,
pubmed-meshheading:19616875-Glucose,
pubmed-meshheading:19616875-Leishmania braziliensis,
pubmed-meshheading:19616875-Leishmaniasis,
pubmed-meshheading:19616875-Macrophages,
pubmed-meshheading:19616875-Mice,
pubmed-meshheading:19616875-Mitochondria,
pubmed-meshheading:19616875-Oxidoreductases,
pubmed-meshheading:19616875-Trypanocidal Agents,
pubmed-meshheading:19616875-Trypanosoma cruzi
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pubmed:year |
2009
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pubmed:articleTitle |
Second generation of 2H-benzimidazole 1,3-dioxide derivatives as anti-trypanosomatid agents: synthesis, biological evaluation, and mode of action studies.
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pubmed:affiliation |
Departamento de Química Orgánica, Facultad de Ciencias-Facultad de Química, Universidad de la República, Igua 4225, 11400 Montevideo, Uruguay.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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