Producción Científica Profesorado

Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain



Alvarez Hernandez, Alejandro

2001

William R. Roush; Jianming Cheng; Beth Knapp-Reed; Alejandro Alvarez-Hernandez; James H. McKerrow; Elizabeth Hansell; Juan C. Engel. Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain. Bioorganic and Medicinal Chemistry Letters, 2001, 11, 2759-2762. ISSN 0960-894X. Pergamon Press, Nueva York. Estados Unidos de América.


Abstract


A new family of potent N-alkoxyvinylsulfonamide inhibitors of cruzain have been developed. Inhibitor 13 has a second order inactivation rate constant of 6,480,000 s?1 M?1 versus cruzain, and is also highly effective against Trypanosoma cruzi trypomastigotes in a tissue culture assay.






Artículos relacionados

ChemInform Abstract: Facile Preparation of [4.4]Metacyclophane- and [5.5]Paracyclophane-Type Macrocy...

Furocoumarins of three species of the genus Dorstenia

Structural studies of spiroarsoranes derived from 2-aminophenols

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

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

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

Diastereomeric C-glycosyloxanthrones from picramnia antidesma

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

Synthesis and Structures of some Lithium and Sodium (Aminoalcoholato)hydrido Aluminates

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