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.






Artículos relacionados

Cathepsins X and B Can Be Differentiated through Their Respective Mono- and Dipeptidyl Carboxypeptid...

r-Alkylation of (S)-Asparagine with Self-Regeneration of the Stereogenic Center: Enantioselective Sy...

Synthesis of new homochiral 2,3-dialkylpiperazines derived from (R)-(?)-phenylglycinol

Synthesis, crystal structures, and quadratic nonlinear optical properties in a series of pushpull bo...

Comparative Structural Characterization of the Biquaternized N-CH3 and N-BH3 Derivatives of the cis-...

Synthesis and Study of Isomeric Benzo[1,4]oxazines and Benzothiazolines by NMR Spectroscopy and X-Ra...

Stereoselective addition of allylmagnesium chloride to the CN bond of [4.3.0] boron heterobicycles

Aroylthioureas: new organic ionophores for heavy-metal ion selective electrodes

Diastereoselective alkylation of chiral glycinate derivatives containing the ?-phenylethyl group.

X-ray crystallographic study of neutral boron chelates with ?-diketones and tropolone