4(1H)-Quinolones with liver stage activity against Plasmodium berghei.

dc.careerCiencias Biológicasen_US
dc.category.authoraddeden_US
dc.contributor.authorSáenz Calderón, Fabián Ernesto
dc.contributor.correspondingLaCrue, Alexis N.en_US
dc.countryEcuadoren_US
dc.date.accessioned2023-11-04T21:33:44Z
dc.date.available2023-11-04T21:33:44Z
dc.date.issued2013
dc.dedication.authorTCen_US
dc.description.abstractWith 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.facultyCiencias Exactas y Naturalesen_US
dc.id.author1706465786en_US
dc.id.type1en_US
dc.identifier.doi10.1128/AAC.00793-12en_US
dc.identifier.issn1098-6596- 0066-4804
dc.identifier.urihttp://aac.asm.org/content/57/1/417.short#aff-1en_US
dc.identifier.urihttps://repositorio.puce.edu.ec/handle/123456789/5218
dc.indexed.databaseOtheren_US
dc.list.authorsLaCrue, 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.pageRange417-424en_US
dc.magazine.titleAntimicrobial Agents Chemotherapyen_US
dc.magazine.volumeChapter57(1)en_US
dc.rightsClosedAccessen_US
dc.statepublisheden_US
dc.subjectQuinolonesen_US
dc.subjectPlasmodium bergheien_US
dc.title4(1H)-Quinolones with liver stage activity against Plasmodium berghei.en_US
Files
Original bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
4 (1H)-Quinolones with Liver Stage Activity.pdf
Size:
2.44 MB
Format:
Adobe Portable Document Format