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dc.contributor.authorWright, Colin W.*
dc.contributor.authorKirby, G.C*
dc.contributor.authorPhillipson, J.D*
dc.contributor.authorWarhurst, D.C.*
dc.contributor.authorLang'at-Thoruwa, C.*
dc.contributor.authorWatt, R.A.*
dc.date.accessioned2009-10-06T08:57:27Z
dc.date.available2009-10-06T08:57:27Z
dc.date.issued2003
dc.identifier.citationWright, C., kirby, G.C., Phillipson, J.D. and Warhurst, D.C. et al. (2003). Enhancement of the antiplasmodial activity of quassin by transformation into a gamma-lactone. Journal of Natural Products. Vol. 66, No. 11, pp. 1486-1489.en
dc.identifier.urihttp://hdl.handle.net/10454/3616
dc.descriptionNoen
dc.description.abstractThe naturally occurring bitter principle quassin (1) was converted chemically into the gamma-lactone quassilactone (13) in an attempt to enhance its antiplasmodial activity. The in vitro antiplasmodial activity of 13 against Plasmodium falciparum (K1) (IC(50) = 23 microM) was 40-fold greater than that of 1. However, one of the intermediates, compound 8, the 15beta-hydroxy,16-O-m-chlorobenzoyl analogue of 1, was 506-fold more active than 1 against P. falciparum (IC(50) = 1.8 microM) and only 3-fold less potent than chloroquine. In addition, 8 displayed the best cytotoxic/antiplasmodial ratio (112) of all of the compounds tested. In the course of this work a dimer, neoquassin ether (6), linked at C-16 was also prepared; 6 was found to have weak antiplasmodial activity (IC(50) = 9.7 microM).en
dc.language.isoenen
dc.relation.isreferencedbyhttp://dx.doi.org/10.1021/np030107aen
dc.subjectBitter principle quassinen
dc.subjectGamma-lactone quassilactoneen
dc.subjectIn vitro antiplasmodialen
dc.subjectQuassinen
dc.titleEnhancement of the antiplasmodial activity of quassin by transformation into a gamma-lactone.en
dc.status.refereedYesen
dc.typeArticleen
dc.type.versionNo full-text available in the repositoryen


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