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Bioorg Med Chem Lett. 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.

Author information

1
Merck Research Laboratories, Kirkland, QC, Canada. beaulieu.ch@videotron.ca

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.

PMID:
21041084
DOI:
10.1016/j.bmcl.2010.10.015
[Indexed for MEDLINE]

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