ABSTRACT
Endochin-like quinolones (ELQs) are potent and specific inhibitors of cytochrome
bc
1
from
Plasmodium falciparum
and
Toxoplasma gondii
and show promise for novel antiparasitic drug development. To determine whether the mitochondrial electron transport chain of
Leishmania
parasites could be targeted similarly for drug development, we investigated the activity of 134 structurally diverse ELQs. A cohort of ELQs was selectively toxic to amastigotes of
Leishmania mexicana
and
L. donovani
, with 50% inhibitory concentrations (IC
50
s) in the low micromolar range, but the structurally similar hydroxynaphthoquinone buparvaquone was by far the most potent inhibitor of electron transport, ATP production, and intracellular amastigote growth. Cytochrome
bc
1
is thus a promising target for novel antileishmanial drugs, and further improvements on the buparvaquone scaffold are warranted for development of enhanced therapeutics.
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