Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease
…, C Mellon, N Méthot, M Ndao, D Nicoll-Griffith…
Index: Beaulieu, Christian; Isabel, Elise; Fortier, Angelique; Masse, Frederic; Mellon, Christophe; Methot, Nathalie; Ndao, Momar; Nicoll-Griffith, Deborah; Lee, Doris; Park, Hyeram; Black, W. Cameron Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7444 - 7449
Full Text: HTML
Citation Number: 25
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.
Related Articles:
[Atkinson, Robert S.; Coogan, Michael P.; Lochrie, Ian S. T. Tetrahedron Letters, 1996 , vol. 37, # 29 p. 5179 - 5182]
[Atkinson, Robert S.; Coogan, Michael P.; Lochrie, Ian S. T. Tetrahedron Letters, 1996 , vol. 37, # 29 p. 5179 - 5182]
[Rossi, Jean-Christophe; Marull, Marc; Boiteau, Laurent; Taillades, Jacques European Journal of Organic Chemistry, 2007 , # 4 p. 662 - 668]
[Atkinson, Robert S.; Coogan, Michael P.; Lochrie, Ian S. T. Tetrahedron Letters, 1996 , vol. 37, # 29 p. 5179 - 5182]