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

Et3B, an Efficient Mediator for Xanthate Transfer Based Radical Processes

Furocoumarins of three species of the genus Dorstenia

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

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

3-Benzoyl-2-isopropyl-4-alkyloxazolidin-5-ones as Efficient and Inexpensive Sources of Enantiopure ?...

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

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

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...

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