1.
Bioorg Med Chem Lett
; 20(24): 7444-9, 2010 Dec 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21041084
RESUMO
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.