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.
Artículos relacionados
Diastereoselective Synthesis of Spiro-?-lactams via Staudinger Reactio
Synthesis of new homochiral 2,3-dialkylpiperazines derived from (R)-(?)-phenylglycinol
Et3, and efficient Mediator for Xanthate Transfer Based Radical Processes.
Diastereoselective alkylation of chiral glycinate derivatives containing the ?-phenylethyl group.
Stereoselective addition of allylmagnesium chloride to the CN bond of [4.3.0] boron heterobicycles
X-ray crystallographic study of neutral boron chelates with ?-diketones and tropolone