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In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes.
- 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