Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10027766 | International Journal of Antimicrobial Agents | 2005 | 6 Pages |
Abstract
Four new chemosensitisers against chloroquine-resistant Plasmodium falciparum based on the 9H-xanthene tricyclic scaffold were designed and synthesised in an attempt to identify simplified compounds that are easily accessible from commercially available starting materials. The compounds contain a common hydrophobic tricyclic 9H-xanthene moiety and an alkyl side chain with two amino groups, one of which is a tertiary substituted terminal amine, separated by three carbons and differing only in the chemical nature of the intermediary nitrogen atom. The best chemosensitising compound has a secondary amino group, showed a response modification index of 0.36 and caused a four-fold increase in chloroquine accumulation in a resistant strain of P. falciparum as well as having the highest selective therapeutic index when tested against a mammalian cell line.
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Authors
Chung-Pu Wu, Donelly A. van Schalkwyk, Dale Taylor, Peter J. Smith, Kelly Chibale,