2. Academic Validation
  3. Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease

Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease

  • J Med Chem. 2012 May 10;55(9):4189-204. doi: 10.1021/jm2015809.
Martine Keenan 1,  Michael J Abbott,  Paul W Alexander,  Tanya Armstrong,  Wayne M Best,  Bradley Berven,  Adriana Botero,  Jason H Chaplin,  Susan A Charman,  Eric Chatelain,  Thomas W von Geldern,  Maria Kerfoot,  Andrea Khong,  Tien Nguyen,  Joshua D McManus,  Julia Morizzi,  Eileen Ryan,  Ivan Scandale,  R Andrew Thompson,  Sen Z Wang,  Karen L White
Affiliations

Affiliation

  • 1 Epichem Pty Ltd, South Street, Murdoch, WA 6150, Australia. martine.keenan@epichem.com.au
PMID: 22536986 DOI: 10.1021/jm2015809
Abstract

We report the discovery of nontoxic fungicide fenarimol (1) as an inhibitor of Trypanosoma cruzi ( T. cruzi ), the causative agent of Chagas disease, and the results of structure-activity investigations leading to potent analogues with low nM IC(50)s in a T. cruzi whole cell in vitro assay. Lead compounds suppressed blood parasitemia to virtually undetectable levels after once daily oral dosing in mouse models of T. cruzi Infection. Compounds are chemically tractable, allowing rapid optimization of target biological activity and drug characteristics. Chemical and biological studies undertaken in the development of the fenarimol series toward the goal of delivering a new drug candidate for Chagas disease are reported.

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