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001-es BibID:	BIBFORM113873
035-os BibID:	(cikkazonosító)12228 (WoS)001041587900021 (Scopus)85165947861
Első szerző:	Bege Miklós (gyógyszerész)
Cím:	In vitro and in vivo antiplasmodial evaluation of sugar-modified nucleoside analogues / Bege Miklós, Singh Vigyasa, Sharma Neha, Debreczeni Nóra, Bereczki Ilona, Herczegh Pál, Rathi Brijesh, Singh Shailja, Borbás Anikó
Dátum:	2023
ISSN:	2045-2322
Megjegyzések:	Drug-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.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk
Megjelenés:	Scientific Reports. - 13 : 1 (2023), p. 1-8 . -
További szerzők:	Singh, Vigyasa Sharma, Neha Debreczeni Nóra (1993-) (vegyész) Bereczki Ilona (1981-) (vegyész, antibiotikumkémikus) Herczegh Pál (1947-) (vegyész, antibiotikumkémikus) Rathi, Brijesh (1986) (vegyész) Singh, Shailja Borbás Anikó (1965-) (vegyész)
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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