Activities of Quinoxaline, Nitroquinoxaline, and [1,2,4]Triazolo[4,3-a]quinoxaline Analogs of MMV007204 against Schistosoma mansoni.

ABSTRACT: The reliance on one drug, praziquantel, to treat the parasitic disease schistosomiasis in millions of people a year shows the need to further develop a pipeline of new drugs to treat this disease. Recently, an antimalarial quinoxaline derivative (MMV007204) from the Medicines for Malaria Venture (MMV) Malaria Box demonstrated promise against Schistosoma mansoni In this study, 47 synthesized compounds containing quinoxaline moieties were first assayed against the larval stage of this parasite, newly transformed schistosomula (NTS); of these, 16 killed over 70% NTS at 10 µM. Further testing against NTS and adult S. mansoni yielded three compounds with 50% inhibitory concentrations (IC₅₀s) of ≤0.31 µM against adult S. mansoni and selectivity indices of ≥8.9. Ad

SUBMITTER: Debbert SL 

PROVIDER: S-EPMC8092513 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature