| Literature DB >> 21041084 |
Christian Beaulieu1, Elise Isabel, Angélique Fortier, Frédéric Massé, Christophe Mellon, Nathalie Méthot, Momar Ndao, Deborah Nicoll-Griffith, Doris Lee, Hyeram Park, W Cameron Black.
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.Entities:
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Year: 2010 PMID： 21041084 DOI： 10.1016/j.bmcl.2010.10.015
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823