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dc.creatorSrbljanović, Jelena
dc.creatorŠtajner, Tijana
dc.creatorKonstantinović, Jelena M.
dc.creatorTerzić-Jovanović, Nataša
dc.creatorUzelac, Aleksandra
dc.creatorBobic, Branko
dc.creatorŠolaja, Bogdan
dc.creatorDjurkovic-Djakovic, Olgica
dc.date.accessioned2019-07-10T13:35:53Z
dc.date.available2018-06-28
dc.date.issued2017
dc.identifier.issn0924-8579
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2172
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/3033
dc.description.abstractMalaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of >= 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo prolonged the survival of treated versus untreated mice, four of which afforded >= 60% survival. Most notably, two of these compounds, both with the adamantane carrier, afforded complete cure (100% survival and parasite clearance). Interestingly, one of these compounds had no in vitro effect against the CQ resistant P. falciparum strain. Better in vivo compared with in vitro results suggest a role for compound metabolites rather than the compounds themselves. The results presented here point to adamantane as a carrier that enhances the antimalarial potential of aminoquinolines.en
dc.publisherElsevier Science Bv, Amsterdam
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.rightsembargoedAccess
dc.sourceInternational Journal of Antimicrobial Agents
dc.subjectMalariaen
dc.subjectAminoquinolinesen
dc.subjectLDH assayen
dc.subjectThompson testen
dc.subjectAdamantaneen
dc.titleExamination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacyen
dc.typearticle
dc.rights.licenseBY-NC-ND
dcterms.abstractКонстантиновиц, Јелена; Србљановиц, Јелена; Стајнер, Тијана; Терзић Јовановић, Наташа; Узелац, Aлександра; Бобиц, Бранко; Шолаја, Богдан; Дјурковиц-Дјаковиц, Олгица;
dc.citation.volume50
dc.citation.issue3
dc.citation.spage461
dc.citation.epage466
dc.citation.other50(3): 461-466
dc.citation.rankM21
dc.description.otherThis is peer-reviewed version of the article: Jelena Srbljanović, Tijana Štajner, Jelena Konstantinović, Nataša Terzić-Jovanović, Aleksandra Uzelac, Branko Bobić, Bogdan A. Šolaja, Olgica Djurković-Djaković, Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy, International Journal of Antimicrobial Agents, 2017, 50, 3, 461-466, [http://dx.doi.org/10.1016/j.ijantimicag.2017.06.002]
dc.description.other[http://cer.ihtm.bg.ac.rs/handle/123456789/2172]
dc.identifier.pmid28668677
dc.identifier.doi10.1016/j.ijantimicag.2017.06.002
dc.identifier.rcubConv_3778
dc.identifier.fulltexthttp://cer.ihtm.bg.ac.rs/bitstream/id/7495/06_10072019_10.1016j.ijantimicag.2017.06.002.pdf
dc.identifier.scopus2-s2.0-85026397158
dc.identifier.wos000408686800025
dc.type.versionacceptedVersion


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