Repurposing the Open Access Malaria Box To Discover Potent Inhibitors of Toxoplasma gondii and Entamoeba histolytica | Zendy

Fabrice Fekam Boyom | Zendy; Patrick Valère Tsouh Fokou | Zendy; Lauve Rachel Yamthe Tchokouaha | Zendy; Thomas Spangenberg | Zendy; Alvine Ngoutane Mfopa | Zendy; Ruffin M. T. Kouipou | Zendy; Cedric Jiatsa Mbouna | Zendy; Valerie Flore Donkeng Donfack | Zendy; P. H. Amvam Zollo | Zendy

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Repurposing the Open Access Malaria Box To Discover Potent Inhibitors of Toxoplasma gondii and Entamoeba histolytica

Author(s) -

Fabrice Fekam Boyom,

Patrick Valère Tsouh Fokou,

Lauve Rachel Yamthe Tchokouaha,

Thomas Spangenberg,

Alvine Ngoutane Mfopa,

Ruffin M. T. Kouipou,

Cedric Jiatsa Mbouna,

Valerie Flore Donkeng Donfack,

P. H. Amvam Zollo

Publication year - 2014

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.02541-14

Subject(s) - entamoeba histolytica , repurposing , toxoplasma gondii , malaria , toxoplasmosis , amoebiasis , biology , pyrimethamine , pharmacology , phenotypic screening , microbiology and biotechnology , virology , plasmodium falciparum , immunology , biochemistry , phenotype , ecology , antibody , gene

Toxoplasmosis and amebiasis are important public health concerns worldwide. The drugs currently available to control these diseases have proven limitations. Therefore, innovative approaches should be adopted to identify and develop new leads from novel scaffolds exhibiting novel modes of action. In this paper, we describe results from the screening of compounds in the Medicines for Malaria Venture (MMV) open access Malaria Box in a search for new anti-Toxoplasma and anti-Entamoeba agents. Standardin vitro phenotypic screening procedures were adopted to assess their biological activities. Seven anti-Toxoplasma compounds with a 50% inhibitory concentration (IC50 ) of 6 were identified. The most interesting compound was MMV007791, a piperazine acetamide, which has an IC50 of 0.19 μM and a selectivity index of >157. Also, we identified two compounds, MMV666600 and MMV006861, with modest activities againstEntamoeba histolytica , with IC50 s of 10.66 μM and 15.58 μM, respectively. The anti-Toxoplasma compounds identified in this study belong to scaffold types different from those of currently used drugs, underscoring their novelty and potential as starting points for the development of new antitoxoplasmosis drugs with novel modes of action.

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