Copy the page URI to the clipboard
Valente, Claudia; Guedes, Rita C.; Moreira, Rui; Iley, Jim; Gut, Jiri and Rosenthal, Philip J.
(2006).
DOI: https://doi.org/10.1016/j.bmcl.2006.04.079
Abstract
The synthesis of phosphonate derivatives of N-phenyl- and N-benzyl-gamma- and delta-sultams, and their application in the Wittig-Horner reaction with N-Boc-L-phenylalanine aldehyde to afford E- and Z-isomers, are described. These compounds were further processed to provide five dipeptide vinyl sultams, which were found to be inactive against papain at concentrations up to 50 microM. In contrast, vinyl sultams demonstrated weak activity against recombinant falcipain-2 and Plasmodium falciparum W2.
Viewing alternatives
Metrics
Public Attention
Altmetrics from AltmetricNumber of Citations
Citations from DimensionsItem Actions
Export
About
- Item ORO ID
- 3982
- Item Type
- Journal Item
- ISSN
- 0960-894X
- Extra Information
- Some of the symbols may not have transferred correctly into this bibliographic record.
- Keywords
- vinylsultams; enzyme inhibition; Wittig–Horner reaction; Vinyl sultams; Papain; Antimalarials; Cysteine proteases; Falcipain-2; Plasmodium falciparum; Molecular modelling
- Academic Unit or School
-
Other Departments > Other Departments
Other Departments - Depositing User
- James Iley