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

Authors
Roush, WR Cheng, JM Knapp-Reed, B Alvarez-Hernandez, A McKerrow, JH Hansell, E Engel, JC
Citation
Wr. Roush et al., Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain, BIOORG MED, 11(20), 2001, pp. 2759-2762
Citations number
40
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
20
Year of publication
2001
Pages
2759 - 2762
Database
ISI
SICI code
0960-894X(20011022)11:20<2759:PSGVSI>2.0.ZU;2-2
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. (C) 2001 Else vier Science Ltd. All rights reserved.