Anti-trypanosomal and antimalarial properties of tetralone derivatives and structurally related benzocycloalkanones
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Date
2019Author
Beteck, Richard M.
Legoabe, Lesetja J.
Isaacs, Michelle
Khanye, Setshaba D.
Laming, Dustin
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Background and objectives: Sleeping sickness and malaria alike are insect-borne protozoan
diseases that share overlapping endemic areas in sub-Saharan Africa. The causative agent for malaria
has developed resistance against all currently deployed anti-malarial agents. In the case of sleeping
sickness, the currently deployed therapeutic options are limited in efficacy and activity spectra, and
there are very few drug candidates in the development pipeline. Thus, there is a need to search for
new drug molecules with a novel mode of actions. Materials and Methods: In the current study, an
in vitro screening of a library of tetralone derivatives and related benzocycloalkanones was effected
against T. b. brucei and P. falciparum. Results: Several hits with low micromolar activity (0.4–8 µM)
against T. b. brucei were identified. Conclusions: The identified hits have a low molecular weight
(<280 Da), a low total polar surface area (<50 Å2
), and a defined structure activity relationship, which
all make them potential starting points for further hit optimization studies
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- Faculty of Health Sciences [2379]