1. Academic Validation
  2. In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes

In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes

  • Bioorg Med Chem Lett. 2020 Nov 15;30(22):127581. doi: 10.1016/j.bmcl.2020.127581.
Janine Aucamp 1 Nonkululeko H Zuma 1 David D N'Da 2
Affiliations

Affiliations

  • 1 Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa.
  • 2 Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa. Electronic address: David.nda@nwu.ac.za.
Abstract

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.

Keywords

Analogue; Artemisinins; Co-infection; Hybrid; Leishmaniasis; Malaria.

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