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

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

Facile synthesis of 1,3,6-oxadiazepines from 2,2?-(1,2-ethanediyldiimino)bisphenols

A practical access to acyl radicals from acyl hydrazides

Et3, and efficient Mediator for Xanthate Transfer Based Radical Processes.

Highly diastereoselective alkylation, acylation and aldol condensation of cis- and trans-(N-acyloyl)...

Synthesis and Study of Monomeric and Dimeric Boronates by Spectroscopic Methods and X-ray Crystallog...

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

Study of the reactivity of squarylferrocenes. Addition of amines and aminoesters

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

Et3B, an Efficient Mediator for Xanthate Transfer Based Radical Processes