Please use this identifier to cite or link to this item: https://cris.library.msu.ac.zw//handle/11408/4922
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dc.contributor.authorTukulula, Matshawandile-
dc.contributor.authorNjoroge, Mathew-
dc.contributor.authorAbay, Efrem T.-
dc.contributor.authorMugumbate, Grace C.-
dc.contributor.authorWiesner, Lubbe-
dc.contributor.authorTaylor, Dale-
dc.contributor.authorGibhard, Liezl-
dc.contributor.authorNorman, Jennifer-
dc.contributor.authorSwart, Kenneth J.-
dc.contributor.authorGut, Jiri-
dc.contributor.authorRosenthal, Philip J.-
dc.contributor.authorBarteau, Samuel-
dc.contributor.authorStreckfuss, Judith-
dc.contributor.authorKameni-Tcheudji, Jacques-
dc.contributor.authorChibale, Kelly-
dc.date.accessioned2022-06-28T12:30:04Z-
dc.date.available2022-06-28T12:30:04Z-
dc.date.issued2013-
dc.identifier.issn1948-5875-
dc.identifier.urihttps://doi.org/10.1021/ml400311r-
dc.identifier.urihttp://hdl.handle.net/11408/4922-
dc.description.abstractA new class of 4-aminoquinolines was synthesized and evaluated in vitro for antiplasmodial activity against both the chloroquine-sensitive (3D7) and -resistant (K1 and W2) strains. The most active compounds 3c–3e had acceptable cytotoxicity but showed strong inhibition toward a panel of cytochrome P450 enzymes in vitro. Pharmacokinetic studies on 3d and 3e in mice showed that they had moderate half-life (4–6 h) and low oral bioavailability. The front runner compound 3d exhibited moderate inhibition of the malaria parasite on P. berghei infected mice following oral administration (5 mg/kg), achieving reduction of parasitemia population by 47% on day 7.en_US
dc.language.isoenen_US
dc.publisherAmerican Chemical Societyen_US
dc.relation.ispartofseriesACS Medicinal Chemistry Letters;Volume 4, No. 12; pages 1198-1202-
dc.subjectAminoquinolinesen_US
dc.subjectantiplasmodial activityen_US
dc.subjectpharmacokineticsen_US
dc.subjectPlasma protein bindingen_US
dc.titleSynthesis and in Vitro and in Vivo Pharmacological Evaluation of New 4-Aminoquinoline-Based Compoundsen_US
dc.typeArticleen_US
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.cerifentitytypePublications-
item.openairetypeArticle-
item.fulltextWith Fulltext-
item.grantfulltextopen-
item.languageiso639-1en-
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