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Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice
dc.creator | Opsenica, Igor | |
dc.creator | Verbić, Tatjana | |
dc.creator | Tot, Mikloš | |
dc.creator | Sciotti, Richard J. | |
dc.creator | Pybus, Brandon S. | |
dc.creator | Đurković-Đaković, Olgica | |
dc.creator | Slavić, Ksenija | |
dc.creator | Šolaja, Bogdan A. | |
dc.date.accessioned | 2018-11-22T00:31:09Z | |
dc.date.available | 2018-11-22T00:31:09Z | |
dc.date.issued | 2015 | |
dc.identifier.issn | 0968-0896 | |
dc.identifier.uri | https://cherry.chem.bg.ac.rs/handle/123456789/1691 | |
dc.description.abstract | We herein report the design and synthesis of a novel series of thiophene-and furan-based aminoquinoline derivatives which were found to be potent antimalarials and inhibitors of b-hematin polymerization. Tested compounds were 3-71 times more potent in vitro than CQ against chloroquine-resistant (CQR) W2 strain with benzonitrile 30 being as active as mefloquine (MFQ), and almost all synthesized aminoquinolines (22/27) were more potent than MFQ against multidrug-resistant (MDR) strain C235. In vivo experiments revealed that compound 28 showed clearance with recrudescence at 40 mg/kg/day, while 5/5 mice survived in Thompson test at 160 mg/kg/day. | en |
dc.publisher | Pergamon-Elsevier Science Ltd, Oxford | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41019/RS// | |
dc.relation | Serbian Academy of Sciences and Arts | |
dc.rights | restrictedAccess | |
dc.source | Bioorganic and Medicinal Chemistry | |
dc.subject | Malaria | en |
dc.subject | Thiophene | en |
dc.subject | Furan | en |
dc.subject | Aminoquinoline inhibitors | en |
dc.subject | P. berghei | en |
dc.subject | Chemotherapy | en |
dc.subject | Cytotoxicity | en |
dc.subject | beta-Hematin polymerization inhibitors | en |
dc.title | Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Опсеница, Игор; Сциотти, Рицхард Ј.; Шолаја, Богдан A.; Славиц, Ксенија; Вербић, Татјана; Дјурковиц-Дјаковиц, Олгица; Пyбус, Брандон С.; Тот, Миклос; | |
dc.citation.volume | 23 | |
dc.citation.issue | 9 | |
dc.citation.spage | 2176 | |
dc.citation.epage | 2186 | |
dc.identifier.wos | 000352698700027 | |
dc.identifier.doi | 10.1016/j.bmc.2015.02.061 | |
dc.citation.other | 23(9): 2176-2186 | |
dc.citation.rank | M22 | |
dc.identifier.pmid | 25801154 | |
dc.description.other | Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3381] | |
dc.type.version | publishedVersion | en |
dc.identifier.scopus | 2-s2.0-84940003621 |