Приказ основних података о документу

dc.creatorOpsenica, Igor
dc.creatorVerbić, Tatjana
dc.creatorTot, Mikloš
dc.creatorSciotti, Richard J.
dc.creatorPybus, Brandon S.
dc.creatorĐurković-Đaković, Olgica
dc.creatorSlavić, Ksenija
dc.creatorŠolaja, Bogdan A.
dc.date.accessioned2018-11-22T00:31:09Z
dc.date.available2018-11-22T00:31:09Z
dc.date.issued2015
dc.identifier.issn0968-0896
dc.identifier.urihttps://cherry.chem.bg.ac.rs/handle/123456789/1691
dc.description.abstractWe 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.publisherPergamon-Elsevier Science Ltd, Oxford
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.relationSerbian Academy of Sciences and Arts
dc.rightsrestrictedAccess
dc.sourceBioorganic and Medicinal Chemistry
dc.subjectMalariaen
dc.subjectThiopheneen
dc.subjectFuranen
dc.subjectAminoquinoline inhibitorsen
dc.subjectP. bergheien
dc.subjectChemotherapyen
dc.subjectCytotoxicityen
dc.subjectbeta-Hematin polymerization inhibitorsen
dc.titleInvestigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure miceen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractОпсеница, Игор; Сциотти, Рицхард Ј.; Шолаја, Богдан A.; Славиц, Ксенија; Вербић, Татјана; Дјурковиц-Дјаковиц, Олгица; Пyбус, Брандон С.; Тот, Миклос;
dc.citation.volume23
dc.citation.issue9
dc.citation.spage2176
dc.citation.epage2186
dc.identifier.wos000352698700027
dc.identifier.doi10.1016/j.bmc.2015.02.061
dc.citation.other23(9): 2176-2186
dc.citation.rankM22
dc.identifier.pmid25801154
dc.description.otherSupplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3381]
dc.type.versionpublishedVersionen
dc.identifier.scopus2-s2.0-84940003621


Документи

Thumbnail

Овај документ се појављује у следећим колекцијама

Приказ основних података о документу