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Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain



Alvarez Hernandez, Alejandro

2001

William R. Roush; Jianming Cheng; Beth Knapp-Reed; Alejandro Alvarez-Hernandez; James H. McKerrow; Elizabeth Hansell; Juan C. Engel. Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain. Bioorganic and Medicinal Chemistry Letters, 2001, 11, 2759-2762. ISSN 0960-894X. Pergamon Press, Nueva York. Estados Unidos de América.


Abstract


A new family of potent N-alkoxyvinylsulfonamide inhibitors of cruzain have been developed. Inhibitor 13 has a second order inactivation rate constant of 6,480,000 s?1 M?1 versus cruzain, and is also highly effective against Trypanosoma cruzi trypomastigotes in a tissue culture assay.





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