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New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton
dc.creator | Opsenica, Igor | |
dc.creator | Opsenica, Dejan | |
dc.creator | Lanteri, C.A. | |
dc.creator | Anova, L. | |
dc.creator | Milhous, Wilbur K. | |
dc.creator | Smith, K. S. | |
dc.creator | Šolaja, Bogdan | |
dc.date.accessioned | 2019-01-30T17:18:29Z | |
dc.date.available | 2019-01-30T17:18:29Z | |
dc.date.issued | 2008 | |
dc.identifier.issn | 0022-2623 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/448 | |
dc.description.abstract | The synthesis of the chimeric molecules consisting of two pharmacophores, tetraoxane and 7-chloro-4-aminoquinoline, is reported. The tetraoxanes 2, 4, and 8 show relatively potent in vitro antimalarial activities, with IC90 values for the Plasmodium falciparum strain W2 of 2.26, 12.44, and 10.74 nM, respectively. In addition, two compounds, 2 and 4, cured mice in a modified Thompson test for antimalarial blood stage activity, with a minimum curative dose of 80 mg/kg, a minimum active dose of 20 mg/kg/day, and a maximum tolerated dose of >960 mg/kg. | en |
dc.publisher | American Chemical Society (ACS) | |
dc.relation | info:eu-repo/grantAgreement/MESTD/MPN2006-2010/142022/RS// | |
dc.rights | restrictedAccess | |
dc.source | Journal of Medicinal Chemistry | |
dc.title | New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Опсеница, Дејан; Опсеница, И.; Милхоус, W.К.; Лантери, Ц.A.; Шолаја, Б.A.; Смитх, К.С.; Aнова, Л.; | |
dc.citation.volume | 51 | |
dc.citation.issue | 19 | |
dc.citation.spage | 6216 | |
dc.citation.epage | 6219 | |
dc.citation.other | 51(19): 6216-6219 | |
dc.citation.rank | aM21 | |
dc.identifier.pmid | 18774792 | |
dc.identifier.doi | 10.1021/jm8006905 | |
dc.identifier.scopus | 2-s2.0-53549086186 | |
dc.identifier.wos | 000259760500040 | |
dc.type.version | publishedVersion |