Discovery of substituted di(pyridin-2-yl)-1,2,4-thiadiazol-5-amines as novel macrofilaricidal compounds for the treatment of human filarial infections

by Hawryluk N, Robinson D, Shen Y, Kyne G, Bedore M, Menon S, Canan S, von Geldern T, Townson S, Gokool S, Ehrens A, Koschel M, Lhermitte-Vallarino N, Martin C, Hoerauf A, Hernandez G, Dalvie D, Specht S, Hübner MP, Scandale I. Journal of Medicinal Chemistry 2022, 65(16);11388-11403. doi: 10.1021/acs.jmedchem.2c00960

Summary: Efforts to control and eliminate onchocerciasis are impeded by a lack of effective treatments that target the adult filarial stage. The authors previously reported a platform using surrogate nematodes in phenotypic ex vivo assays to assess activity across various parasites, which led to a series of amino-thiazole molecules demonstrating ex vivo killing of adult O. gutturosa, B. malayi, B. pahangi, and L. sigmodontis. Following on from this, in this manuscript, the authors describe the discovery of a series of substituted di(pyridin-2-yl)- 1,2,4-thiadiazol-5-amines as novel macrofilaricides for the treatment of human filarial infections.

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