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Expeditious synthesis and biological evaluation of novel 2,N6-disubstituted 1,2 dihydro-1,3,5-triazine-4,6-diamines as potential antimalarials

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dc.contributor.author Gravestock, David
dc.contributor.author Rousseau, Amanda L.
dc.contributor.author Lourens, Anna Catharina U.
dc.contributor.author Moleele, Simon S.
dc.contributor.author Van Zyl, Robyn L.
dc.contributor.author Steenkamp, Paul A.
dc.date.accessioned 2012-10-04T07:04:15Z
dc.date.available 2012-10-04T07:04:15Z
dc.date.issued 2011
dc.identifier.citation Gravestock, 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.issn 0223-5234
dc.identifier.issn 1768-3254 (Online)
dc.identifier.uri http://hdl.handle.net/10394/7437
dc.description Published under the auspices of the French Société de Chimie Thérapeutique (SCT) en_US
dc.description.abstract A 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.iso en en_US
dc.subject Cycloguanil en_US
dc.subject biguanide en_US
dc.subject 2,N6-disubstituted 1,2-dihydro-1,3,5-triazine-4,6-diamine en_US
dc.subject antimalarial en_US
dc.subject FCR-3 plasmodium falciparum strain en_US
dc.title Expeditious synthesis and biological evaluation of novel 2,N6-disubstituted 1,2 dihydro-1,3,5-triazine-4,6-diamines as potential antimalarials en_US
dc.type Article en_US


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