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. 2010 Dec 15;20(24):7444-9.
doi: 10.1016/j.bmcl.2010.10.015. Epub 2010 Oct 12.

Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease

Christian Beaulieu  1 , Elise Isabel, Angélique Fortier, Frédéric Massé, Christophe Mellon, Nathalie Méthot, Momar Ndao, Deborah Nicoll-Griffith, Doris Lee, Hyeram Park, W Cameron Black
Affiliations

Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease

Christian Beaulieu et al. Bioorg Med Chem Lett. .

Abstract

Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease is described. The identified inhibitors bearing an amino nitrile warhead in P1 exhibit low nanomolar in vitro potency against cruzipain. Further SAR in P2 portion led to the identification of compounds, such as 26, that have a unique selectivity profile against other cysteine proteases and offering new opportunities for safer treatment of Chagas disease.

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