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- Carrasco, MartaGothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology (author)
Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites
- Article/chapterEnglish2016
Publisher, publication year, extent ...
- 2016-08-19
- Wiley,2016
Numbers
- LIBRIS-ID:oai:gup.ub.gu.se/246469
- https://gup.ub.gu.se/publication/246469URI
- https://doi.org/10.1002/cmdc.201600327DOI
Supplementary language notes
- Language:English
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Notes
- 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 and genre
- NATURVETENSKAP Biologi Biokemi och molekylärbiologi hsv//swe
- NATURAL SCIENCES Biological Sciences Biochemistry and Molecular Biology hsv//eng
- antiprotozoal agents
- azaaurones
- erythrocytic stage
- liver stage
- malaria
- cysteine protease inhibitors
- plasmodium-falciparum
- liver-stage
- selective inhibitors
- antimalarial-drug
- discovery
- potent
- mechanisms
- resistance
- aurones
Added entries (persons, corporate bodies, meetings, titles ...)
- Machado, M. (author)
- Goncalves, L. (author)
- Sharma, M. (author)
- Gut, J. (author)
- Lukens, A. K. (author)
- Wirth, D. F. (author)
- Andre, V. (author)
- Duarte, M. T. (author)
- Guedes, R. C. (author)
- dos Santos, Djva (author)
- Rosenthal, P. J. (author)
- Mazitschek, R. (author)
- Prudencio, M. (author)
- Moreira, R. (author)
- Göteborgs universitetInstitutionen för kemi och molekylärbiologi (creator_code:org_t)
Related titles
- In:Chemmedchem: Wiley11:19, s. 2194-22041860-7179
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- Wirth, D. F.
- Andre, V.
- Duarte, M. T.
- Guedes, R. C.
- dos Santos, Djva
- Rosenthal, P. J.
- Mazitschek, R.
- Prudencio, M.
- Moreira, R.
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