Discovery of Substituted Di(pyridin-2-yl)-1,2,4-thiadiazol-5-amines as Novel Macrofilaricidal Compounds for the Treatment of Human Filarial Infections

Filarial diseases, including lymphatic filariasis and onchocerciasis, are considered among the most devastating of all tropical diseases, affecting about 145 million people worldwide. Efforts to control and eliminate onchocerciasis are impeded by a lack of effective treatments that target the adult...

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Published inJournal of medicinal chemistry Vol. 65; no. 16; pp. 11388 - 11403
Main Authors Hawryluk, Natalie, Robinson, Dale, Shen, Yixing, Kyne, Graham, Bedore, Matthew, Menon, Sanjay, Canan, Stacie, von Geldern, Thomas, Townson, Simon, Gokool, Suzanne, Ehrens, Alexandra, Koschel, Marianne, Lhermitte-Vallarino, Nathaly, Martin, Coralie, Hoerauf, Achim, Hernandez, Geraldine, Dalvie, Deepak, Specht, Sabine, Hübner, Marc Peter, Scandale, Ivan
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 25.08.2022
Amer Chemical Soc
Subjects
Chemical Sciences
Chemistry, Medicinal
Life Sciences
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
MEDIATED EFFLUX
IMPACT
GLYCOPROTEIN
LIGAND EFFICIENCY
PERMEABILITY
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Summary:Filarial diseases, including lymphatic filariasis and onchocerciasis, are considered among the most devastating of all tropical diseases, affecting about 145 million people worldwide. Efforts to control and eliminate onchocerciasis are impeded by a lack of effective treatments that target the adult filarial stage. Herein, we 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.
Bibliography:ObjectType-Article-1
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ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.2c00960