WFRF:(Wirth T)
Sökning: WFRF:(Wirth T) > (2015-2019) > Probing the Azaauro...
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| Fältnamn | Indikatorer | Metadata |
|---|---|---|
| 000 | 03301naa a2200625 4500 | |
| 001 | oai:gup.ub.gu.se/246469 | |
| 003 | SwePub | |
| 008 | 240910s2016 | |||||||||||000 ||eng| | |
| 024 | 7 | a https://gup.ub.gu.se/publication/2464692 URI |
| 024 | 7 | a https://doi.org/10.1002/cmdc.2016003272 DOI |
| 040 | a (SwePub)gu | |
| 041 | a eng | |
| 042 | 9 SwePub | |
| 072 | 7 | a ref2 swepub-contenttype |
| 072 | 7 | a art2 swepub-publicationtype |
| 100 | 1 | a Carrasco, Martau Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology4 aut |
| 245 | 1 0 | a Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites |
| 264 | c 2016-08-19 | |
| 264 | 1 | b Wiley,c 2016 |
| 520 | a 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. | |
| 650 | 7 | a NATURVETENSKAPx Biologix Biokemi och molekylärbiologi0 (SwePub)106022 hsv//swe |
| 650 | 7 | a NATURAL SCIENCESx Biological Sciencesx Biochemistry and Molecular Biology0 (SwePub)106022 hsv//eng |
| 653 | a antiprotozoal agents | |
| 653 | a azaaurones | |
| 653 | a erythrocytic stage | |
| 653 | a liver stage | |
| 653 | a malaria | |
| 653 | a cysteine protease inhibitors | |
| 653 | a plasmodium-falciparum | |
| 653 | a liver-stage | |
| 653 | a selective inhibitors | |
| 653 | a antimalarial-drug | |
| 653 | a discovery | |
| 653 | a potent | |
| 653 | a mechanisms | |
| 653 | a resistance | |
| 653 | a aurones | |
| 700 | 1 | a Machado, M.4 aut |
| 700 | 1 | a Goncalves, L.4 aut |
| 700 | 1 | a Sharma, M.4 aut |
| 700 | 1 | a Gut, J.4 aut |
| 700 | 1 | a Lukens, A. K.4 aut |
| 700 | 1 | a Wirth, D. F.4 aut |
| 700 | 1 | a Andre, V.4 aut |
| 700 | 1 | a Duarte, M. T.4 aut |
| 700 | 1 | a Guedes, R. C.4 aut |
| 700 | 1 | a dos Santos, Djva4 aut |
| 700 | 1 | a Rosenthal, P. J.4 aut |
| 700 | 1 | a Mazitschek, R.4 aut |
| 700 | 1 | a Prudencio, M.4 aut |
| 700 | 1 | a Moreira, R.4 aut |
| 710 | 2 | a Göteborgs universitetb Institutionen för kemi och molekylärbiologi4 org |
| 773 | 0 | t Chemmedchemd : Wileyg 11:19, s. 2194-2204q 11:19<2194-2204x 1860-7179 |
| 856 | 4 8 | u https://gup.ub.gu.se/publication/246469 |
| 856 | 4 8 | u https://doi.org/10.1002/cmdc.201600327 |
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- Andre, V.
- Duarte, M. T.
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