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dc.creatorSrbljanović, Jelena
dc.creatorBobić, Branko
dc.creatorŠtajner, Tijana
dc.creatorUzelac, Aleksandra
dc.creatorOpsenica, Igor
dc.creatorTerzić-Jovanović, Nataša
dc.creatorBauman, Neda
dc.creatorŠolaja, Bogdan
dc.creatorĐurković-Đaković, Olgica
dc.date.accessioned2021-04-20T13:06:28Z
dc.date.available2021-04-20T13:06:28Z
dc.date.issued2020
dc.identifier.issn2213-7165
dc.identifier.urihttp://rimi.imi.bg.ac.rs/handle/123456789/998
dc.description.abstractObjectives: Malaria treatment is impeded by increasing resistance to conventional antimalarial drugs. Here we explored the activity of ten novel benzothiophene, thiophene and benzene aminoquinolines. Methods: In vitro testing was performed by the lactate dehydrogenase assay in chloroquine (CQ)-sensitive Plasmodium falciparum strain 3D7 and CQ-resistant (CQ(R)) P. falciparum strain Dd2. In vivo activity was evaluated by a modified Thompson test using C57BL/6 mice infected with Plasmodium berghei ANKA strain. Results: Nine of the ten compounds had a lower 50% inhibitory concentration (IC50) than CQ against the CQ(R) strain Dd2. Five of these compounds that were available for in vivo evaluation were shown to be nontoxic. All five compounds administered at a dose of 160 mg/kg/day for 3 days prolonged the survival of treated compared with untreated mice. Untreated control mice died by Day 7 with a mean parasitaemia of 15%. Among treated mice, a dichotomous outcome was observed, with a two-third majority of treated mice dying by Day 17 with a low mean parasitaemia of 5%, whilst one-third survived longer with a mean hyperparasitaemia of 70%; specifically, five of these mice survived a mean of 25 days, whilst two even survived past Day 31. Conclusions: The significant antimalarial potential of this aminoquinoline series is illustrated by its excellent in vitro activity against the CQ(R) P. falciparum strain and significant in vivo activity. Interestingly, compounds CIAQ7, CIAQ9 and CIAQ11 were able to confer resistance to cerebral malaria and afford a switch to hyperparasitaemia to mice prone to the neurological syndrome.en
dc.publisherElsevier Sci Ltd, Oxford
dc.relationinfo:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41019/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS//
dc.rightsopenAccess
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/4.0/
dc.sourceJournal of Global Antimicrobial Resistance
dc.subjectMalariaen
dc.subjectAminoquinolinesen
dc.subjectPlasmodium bergheien
dc.subjectC57BL/6 miceen
dc.subjectHyperparasitaemiaen
dc.titleAminoquinolines afford resistance to cerebral malaria in susceptible miceen
dc.typearticle
dc.rights.licenseBY-NC-ND
dc.citation.epage25
dc.citation.other23: 20-25
dc.citation.rankM22~
dc.citation.spage20
dc.citation.volume23
dc.identifier.doi10.1016/j.jgar.2020.07.027
dc.identifier.fulltexthttp://rimi.imi.bg.ac.rs/bitstream/id/796/995.pdf
dc.identifier.pmid32810640
dc.identifier.scopus2-s2.0-85090019754
dc.identifier.wos000604981100005
dc.type.versionpublishedVersion


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