Приказ основних података о документу

dc.creatorKonstantinović, Jelena
dc.creatorVidenović, Milica
dc.creatorSrbljanović, Jelena
dc.creatorĐurković-Đaković, Olgica
dc.creatorBogojević, Katarina
dc.creatorSciotti, Richard J.
dc.creatorŠolaja, Bogdan
dc.date.accessioned2021-04-20T12:54:00Z
dc.date.available2021-04-20T12:54:00Z
dc.date.issued2017
dc.identifier.issn1420-3049
dc.identifier.urihttp://rimi.imi.bg.ac.rs/handle/123456789/803
dc.description.abstractMalaria is a severe and life-threatening disease caused by Plasmodium parasites that are spread to humans through bites of infected Anopheles mosquitoes. Here, we report on the efficacy of aminoquinolines coupled to benzothiophene and thiophene rings in inhibiting Plasmodium falciparum parasite growth. Synthesized compounds were evaluated for their antimalarial activity and toxicity, in vitro and in mice. Benzothiophenes presented in this paper showed improved activities against a chloroquine susceptible (CQS) strain, with potencies of IC50 = 6 nM, and cured 5/5 Plasmodium berghei infected mice when dosed orally at 160 mg/kg/day x 3 days. In the benzothiophene series, the examined antiplasmodials were more active against the CQS strain D6, than against strains chloroquine resistant (CQR) W2 and multidrug-resistant (MDR) TM91C235. For the thiophene series, a very interesting feature was revealed: hypersensitivity to the CQR strains, resistance index (RI) of lt 1. This is in sharp contrast to chloroquine, indicating that further development of the series would provide us with more potent antimalarials against CQR strains.en
dc.publisherMDPI, Basel
dc.relationSerbian Academy of Sciences and Arts
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41019/RS//
dc.rightsopenAccess
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.sourceMolecules
dc.subjectantimalarialsen
dc.subjectthiopheneen
dc.subjectbenzothiopheneen
dc.subjectaminoquinolineen
dc.titleAntimalarials with Benzothiophene Moieties as Aminoquinoline Partnersen
dc.typearticle
dc.rights.licenseBY
dc.citation.issue3
dc.citation.other22(3): -
dc.citation.rankM22
dc.citation.spage343
dc.citation.volume22
dc.identifier.doi10.3390/molecules22030343
dc.identifier.fulltexthttp://rimi.imi.bg.ac.rs/bitstream/id/616/800.pdf
dc.identifier.pmid28245583
dc.identifier.scopus2-s2.0-85014450786
dc.identifier.wos000398743500004
dc.type.versionpublishedVersion


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Приказ основних података о документу