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In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.

Authors :
Aucamp, Janine
Zuma, Nonkululeko H.
N'Da, David D.
Source :
Bioorganic & Medicinal Chemistry Letters. Nov2020, Vol. 30 Issue 22, pN.PAG-N.PAG. 1p.
Publication Year :
2020

Abstract

• Antiplasmodial active artemisinins screened against various Leishmania strains. • Several antipromastigote hits. • Leishmania were less susceptible to artemisinin derivatives than Plasmodia. • Promising anti-coinfection hits. 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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
0960894X
Volume :
30
Issue :
22
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
147117885
Full Text :
https://doi.org/10.1016/j.bmcl.2020.127581