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

Synthesis of nitrogen-, oxygen- and sulphur-containing tripodal ligands with a trimethylbenzene core...

Phenylboronic acid catalyzed-cyanide promoted, one-pot synthesis of 2-(2-hydroxyphenyl)benzoxazole d...

Phenylboronic acid catalyzed-cyanide promoted, one-pot synthesis of 2-(2-hydroxyphenyl)benzoxazole d...

Enantioselective synthesis of ?-amino acids. Part 10: Preparation of novel ?,?- and ?,?-disubstitute...

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

Phenylmethyl 2,3,4-tri-O-acetyl--D-fucopyranoside

Preparation of Seven- and Eight-Membered Boron Heterocycles from Different Salen Ligands and Arylbor...

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

Preparation of N-aryl-substituted spiro-?-lactams via Staudinger cycloaddition

Diastereomeric C-glycosyloxanthrones from picramnia antidesma