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

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

Further insight into three center hydrogen bonding. Participation in tautomeric equilibria of hetero...

Addition reaction of benzylbenzylidenenamine to lithium enolates of1,3-dioxolan-4-one: synthesis of ...

A practical access to acyl radicals from acyl hydrazides

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

Enantioselective synthesis of ?-amino acids. Part 11: Diastereoselective alkylation of chiral deriva...

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

A flexible access to highly functionalised boronates

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

An efficient potassium cyanide-promoted synthesis of 2-arylbenzoxazoles from [4.3.0]boron heterobicy...