Novel naphthoquinone derivatives: Synthesis and activity against human African trypanosomiasis |
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Authors: | Bhupesh S. Samant Chikomborero Chakaingesu |
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Affiliation: | Natural Product and Medicinal Chemistry (NPMC) Research Group, Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Rhodes University, Grahamstown 6140, South Africa |
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Abstract: | A series of naphthoquinone derivatives has been synthesized and tested for its biological activity against human African trypanosomiasis. The use of reverse micellar medium not only enhanced the conversion rate, but also showed selectivity towards mono-coupled product in aryl chloride–aniline coupling reactions. Two derivatives of naphthoquinone (9b and 9c) exhibited potent activity against Trypanosoma brucei in vitro with low cytotoxicity. |
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