4(1H)-Quinolones with liver stage activity against Plasmodium berghei.
dc.career | Ciencias Biológicas | en_US |
dc.category.author | added | en_US |
dc.contributor.author | Sáenz Calderón, Fabián Ernesto | |
dc.contributor.corresponding | LaCrue, Alexis N. | en_US |
dc.country | Ecuador | en_US |
dc.date.accessioned | 2023-11-04T21:33:44Z | |
dc.date.available | 2023-11-04T21:33:44Z | |
dc.date.issued | 2013 | |
dc.dedication.author | TC | en_US |
dc.description.abstract | With the exception of primaquine, tafenoquine, and atovaquone, there are very few antimalarials that target liver stage parasites. In this study, a transgenic Plasmodium berghei parasite (1052Cl1; PbGFP-Luccon) that expresses luciferase was used to assess the anti-liver stage parasite activity of ICI 56,780, a 7-(2-phenoxyethoxy)-4(1H)-quinolone (PEQ), as well as two 3-phenyl-4(1H)-quinolones (P4Q), P4Q-146 and P4Q-158, by using bioluminescent imaging (BLI). Results showed that all of the compounds were active against liver stage parasites; however, ICI 56,780 and P4Q-158 were the most active, with low nanomolar activity in vitro and causal prophylactic activity in vivo. This potent activity makes these compounds ideal candidates for advancement as novel antimalarials. | en_US |
dc.faculty | Ciencias Exactas y Naturales | en_US |
dc.id.author | 1706465786 | en_US |
dc.id.type | 1 | en_US |
dc.identifier.doi | 10.1128/AAC.00793-12 | en_US |
dc.identifier.issn | 1098-6596- 0066-4804 | |
dc.identifier.uri | http://aac.asm.org/content/57/1/417.short#aff-1 | en_US |
dc.identifier.uri | https://repositorio.puce.edu.ec/handle/123456789/5218 | |
dc.indexed.database | Other | en_US |
dc.list.authors | LaCrue, A. N., Sáenz, F. E., Cross, R. M., Udenze, K. O., Monastyrskyi, A., Stein, S., Mutka, T. S., Manetsch, R., Kyle, D. E. | en_US |
dc.magazine.pageRange | 417-424 | en_US |
dc.magazine.title | Antimicrobial Agents Chemotherapy | en_US |
dc.magazine.volumeChapter | 57(1) | en_US |
dc.rights | ClosedAccess | en_US |
dc.state | published | en_US |
dc.subject | Quinolones | en_US |
dc.subject | Plasmodium berghei | en_US |
dc.title | 4(1H)-Quinolones with liver stage activity against Plasmodium berghei. | en_US |
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