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dc.contributor.authorGravestock, David
dc.contributor.authorRousseau, Amanda L.
dc.contributor.authorLourens, Anna Catharina U.
dc.contributor.authorMoleele, Simon S.
dc.contributor.authorVan Zyl, Robyn L.
dc.contributor.authorSteenkamp, Paul A.
dc.date.accessioned2012-10-04T07:04:15Z
dc.date.available2012-10-04T07:04:15Z
dc.date.issued2011
dc.identifier.citationGravestock, D. et al. 2011. Expeditious synthesis and biological evaluation of novel 2,N6-disubstituted 1,2 dihydro-1,3,5-triazine-4,6-diamines as potential antimalarials. European journal of medicinal chemistry, 46(6):2022-2030. [http://www.journals.elsevier.com/european-journal-of-medicinal-chemistry/]en_US
dc.identifier.issn0223-5234
dc.identifier.issn1768-3254 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/7437
dc.descriptionPublished under the auspices of the French Société de Chimie Thérapeutique (SCT)en_US
dc.description.abstractA small set of novel 2,N6-disubstituted 1,2-dihydro-1,3,5-triazine-4,6-diamines was prepared possessing a flexible tether between the exocyclic nitrogen bonded to C-6 of the 1,2-dihydro-1,3,5-triazine-4,6-diamine heterocycle and the distal aryl ring. Three zones were varied in this series of compounds, namely the nature of the substituent(s) on C-2; the nature of the substituent(s) on the distal aryl ring; as well as the nature and length of the flexible tether between the rings. The compound showing the best antimalarial activity (cycloguanil-resistant FCR-3 Plasmodium falciparum IC50 ¼ 0.99 mM) was N6-(3-(4-chlorophenoxy)propyl)-2-(furan-2-yl)-1,2-dihydro-1,3,5-triazine-4,6-diamine hydrochloride.en_US
dc.language.isoenen_US
dc.subjectCycloguanilen_US
dc.subjectbiguanideen_US
dc.subject2,N6-disubstituted 1,2-dihydro-1,3,5-triazine-4,6-diamineen_US
dc.subjectantimalarialen_US
dc.subjectFCR-3 plasmodium falciparum strainen_US
dc.titleExpeditious synthesis and biological evaluation of novel 2,N6-disubstituted 1,2 dihydro-1,3,5-triazine-4,6-diamines as potential antimalarialsen_US
dc.typeArticleen_US


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