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Probing the Azaauro...
Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites
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- Carrasco, Marta (author)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology
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Machado, M. (author)
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Goncalves, L. (author)
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Sharma, M. (author)
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Gut, J. (author)
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Lukens, A. K. (author)
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Wirth, D. F. (author)
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Andre, V. (author)
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Duarte, M. T. (author)
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Guedes, R. C. (author)
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dos Santos, Djva (author)
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Rosenthal, P. J. (author)
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Mazitschek, R. (author)
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Prudencio, M. (author)
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Moreira, R. (author)
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(creator_code:org_t)
- 2016-08-19
- 2016
- English.
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In: Chemmedchem. - : Wiley. - 1860-7179. ; 11:19, s. 2194-2204
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Abstract
Subject headings
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- The potential of azaaurones as dual-stage antimalarial agents was investigated by assessing the effect of a small library of azaaurones on the inhibition of liver and intraerythrocytic lifecycle stages of the malaria parasite. The whole series was screened against the blood stage of a chloroquine-resistant Plasmodium falciparum strain and the liver stage of P.berghei, yielding compounds with dual-stage activity and sub-micromolar potency against erythrocytic parasites. Studies with genetically modified parasites, using a phenotypic assay based on the P.falciparum Dd2-ScDHODH line, which expresses yeast dihydroorotate dehydrogenase (DHODH), showed that one of the azaaurone derivatives has the potential to inhibit the parasite mitochondrial electron-transport chain. The global urgency in finding new therapies for malaria, especially against the underexplored liver stage, associated with chemical tractability of azaaurones, warrants further development of this chemotype. Overall, these results emphasize the azaaurone chemotype as a promising scaffold for dual-stage antimalarials.
Subject headings
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
Keyword
- antiprotozoal agents
- azaaurones
- erythrocytic stage
- liver stage
- malaria
- cysteine protease inhibitors
- plasmodium-falciparum
- liver-stage
- selective inhibitors
- antimalarial-drug
- discovery
- potent
- mechanisms
- resistance
- aurones
Publication and Content Type
- ref (subject category)
- art (subject category)
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To the university's database
- By the author/editor
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Carrasco, Marta
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Machado, M.
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Goncalves, L.
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Sharma, M.
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Gut, J.
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Lukens, A. K.
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show more...
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Wirth, D. F.
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Andre, V.
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Duarte, M. T.
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Guedes, R. C.
-
dos Santos, Djva
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Rosenthal, P. J.
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Mazitschek, R.
-
Prudencio, M.
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Moreira, R.
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show less...
- About the subject
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Biological Scien ...
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and Biochemistry and ...
- Articles in the publication
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Chemmedchem
- By the university
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University of Gothenburg