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Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents |
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| Authors: | Kelly Chibale Mark VisserDonelly van Schalkwyk Peter J SmithAhilan Saravanamuthu Alan H Fairlamb |
| Affiliation: | a Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa b Division of Pharmacology, Department of Medicine, University of Cape Town Medical School, Observatory 7925, South Africa c Division of Biological Chemistry and Molecular Microbiology, School of Life Sciences, Wellcome Trust Biocentre, University of Dundee, Dundee DD1 5EH, UK |
| Abstract: | Xanthene derivatives were synthesized and evaluated for their potential as trypanothione reductase (TryR) inhibitors and chloroquine (CQ) potentiating agents. Some derivatives displayed inhibitory activity against TryR comparable to known tricyclic anti-depressants. On the other hand a number of derivatives increased CQ accumulation and potentiating effects in a resistant strain of Plasmodium falciparum with one compound also displaying strong intrinsic antimalarial activity. |
| Keywords: | 9,9-dimethylxanthenes trypanothione reductase inhibitors chloroquine potentiating agents trypanosomiasis leishmaniasis malaria |
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