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

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

  • J Med Chem. 2022 Aug 25;65(16):11388-11403. doi: 10.1021/acs.jmedchem.2c00960.
Natalie Hawryluk 1,  Dale Robinson 1,  Yixing Shen 1,  Graham Kyne 2,  Matthew Bedore 2,  Sanjay Menon 2,  Stacie Canan 1,  Thomas von Geldern 3,  Simon Townson 4,  Suzanne Gokool 4,  Alexandra Ehrens 5 6,  Marianne Koschel 5,  Nathaly Lhermitte-Vallarino 7,  Coralie Martin 7,  Achim Hoerauf 5 6,  Geraldine Hernandez 1,  Deepak Dalvie 1,  Sabine Specht 5 8,  Marc Peter Hübner 5 6,  Ivan Scandale 8
Affiliations

Affiliations

  • 1 Bristol Myers Squibb, San Diego, California 92121, United States.
  • 2 Zoetis, Kalamazoo, Michigan 49001, United States.
  • 3 Embedded Consulting, Richmond, Illinois 60071, United States.
  • 4 Northwick Park Institute for Medical Research, London HA1 3UJ, UK.
  • 5 Institute for Medical Microbiology, Immunology & Parasitology, University Hospital Bonn, 53127 Bonn, Germany.
  • 6 German Center for Infection Research (DZIF), partner site Bonn-Cologne, 53127 Bonn, Germany.
  • 7 Unité Molécules de Communication et Adaptation des Microorganismes (MCAM, UMR 7245), Muséum national d'Histoire Naturelle, Paris 75005, France.
  • 8 Drugs for Neglected Diseases Initiative, Geneva 1204, Switzerland.
PMID: 35972896 DOI: 10.1021/acs.jmedchem.2c00960
Abstract

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.

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