Producción Científica Profesorado

Design, Synthesis and Evaluation of d-Homophenylalanyl Epoxysuccinate Inhibitors of the Trypanosomal Cysteine Protease Cruzain



Alvarez Hernandez, Alejandro

2000

William R. Roush, Alejandro Alvarez Hernández, James H. McKerrow, Paul M. Selzer, Elizabeth Hansell and Juan C. Engel. Design, Synthesis and Evaluation of D-Homophenylalanyl Epoxysuccinate Inhibitors of the Trypanosomal Cysteine Protease Cruzain. Tetrahedron, 2000, 56, 9747-9762. ISNN 0040-40200563-2064. Pergamon Press New York, Estados Unidos de America.


Abstract


The binding modes of E-64c to papain combined with molecular modeling and ligand design using the crystal structure of cruzain have been used to develop new, potent d-Homophenylalanyl epoxysuccinate inhibitors of cruzain, the major cysteine protease of Trypanosoma cruzi. The most potent inhibitor 47 contains an O-benzyl hydroxamate unit and is highly specific for cruzain relative to other cysteine proteases tested.






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