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In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes

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Leishmaniasis is a neglected tropical disease affecting thousands worldwide, especially in developing countries where it co-exists with malaria. Only a handful of drugs are clinically available to treat the disease, but significant limitations threaten their very use. New, safe and effective drugs, including those against malaria-leishmaniasis co-infections, are thus imperative. We assessed the in vitro anti-infective potential of previously synthesized, potent antimalarial artemisinin derivatives. Analogue esters featuring 1,1′-biphenyl and thiophenyl moieties were as much as 30-fold more potent than clinical artemisinins against L. donovani parasites, qualifying them as antipromastigote hits for further investigation in the search for malaria-leishmaniasis co-infection therapies

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Aucamp, J. et al. 2020. In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes. Bioorganic and medicinal chemistry letters, 30(22):Art. #127581. [https://doi.org/10.1016/j.bmcl.2020.127581]

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