Show simple item record

dc.contributor.authorBege, M.
dc.contributor.authorSingh, V.
dc.contributor.authorSharma, N.
dc.contributor.authorDebreczeni, N.
dc.contributor.authorBereczki, I.
dc.contributor.authorPoonam
dc.contributor.authorHerczegh, P.
dc.contributor.authorRathi, B.
dc.contributor.authorSingh, S.
dc.contributor.authorBorbás, A.
dc.date.accessioned2024-08-06T03:49:48Z
dc.date.available2024-08-06T03:49:48Z
dc.date.issued2023-07-28
dc.identifier.citationBege, M., Singh, V., Sharma, N. et al. In vitro and in vivo antiplasmodial evaluation of sugar-modified nucleoside analogues. Sci Rep 13, 12228 (2023). https://doi.org/10.1038/s41598-023-39541-4
dc.identifier.issn2045-2322
dc.identifier.pmid37507429
dc.identifier.doi10.1038/s41598-023-39541-4
dc.identifier.urihttp://hdl.handle.net/10150/673838
dc.description.abstractDrug-resistant Plasmodium falciparum (Pf) infections are a major burden on the population and the healthcare system. The establishment of Pf resistance to most existing antimalarial therapies has complicated the problem, and the emergence of resistance to artemisinin derivatives is even more concerning. It is increasingly difficult to cure malaria patients due to the limited availability of effective antimalarial drugs, resulting in an urgent need for more efficacious and affordable treatments to eradicate this disease. Herein, new nucleoside analogues including morpholino-nucleoside hybrids and thio-substituted nucleoside derivatives were prepared and evaluated for in vitro and in vivo antiparasitic activity that led a few hits especially nucleoside-thiopyranoside conjugates, which are highly effective against Pf3D7 and PfRKL-9 strains in submicromolar concentration. One adenosine derivative and four pyrimidine nucleoside analogues significantly reduced the parasite burden in mouse models infected with Plasmodium berghei ANKA. Importantly, no significant hemolysis and cytotoxicity towards human cell line (RAW) was observed for the hits, suggesting their safety profile. Preliminary research suggested that these thiosugar-nucleoside conjugates could be used to accelerate the antimalarial drug development pipeline and thus deserve further investigation. © 2023, The Author(s).
dc.language.isoen
dc.publisherNature Research
dc.rights© The Author(s) 2023. This article is licensed under a Creative Commons Attribution 4.0 International License.
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.titleIn vitro and in vivo antiplasmodial evaluation of sugar-modified nucleoside analogues
dc.typeArticle
dc.typetext
dc.contributor.departmentDepartment of Pharmacology and Toxicology, College of Pharmacy, University of Arizona
dc.identifier.journalScientific Reports
dc.description.noteOpen access journal
dc.description.collectioninformationThis item from the UA Faculty Publications collection is made available by the University of Arizona with support from the University of Arizona Libraries. If you have questions, please contact us at repository@u.library.arizona.edu.
dc.eprint.versionFinal Published Version
dc.source.journaltitleScientific Reports
refterms.dateFOA2024-08-06T03:49:48Z


Files in this item

Thumbnail
Name:
s41598-023-39541-4.pdf
Size:
2.026Mb
Format:
PDF
Description:
Final Published Version

This item appears in the following Collection(s)

Show simple item record

© The Author(s) 2023. This article is licensed under a Creative Commons Attribution 4.0 International License.
Except where otherwise noted, this item's license is described as © The Author(s) 2023. This article is licensed under a Creative Commons Attribution 4.0 International License.