Valente, Claudia; Guedes, Rita C.; Moreira, Rui; Iley, Jim; Gut, Jiri and Rosenthal, Philip J.
|DOI (Digital Object Identifier) Link:||http://doi.org/10.1016/j.bmcl.2006.04.079|
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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.
|Item Type:||Journal Article|
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|Keywords:||vinylsultams; enzyme inhibition; Wittig–Horner reaction; Vinyl sultams; Papain; Antimalarials; Cysteine proteases; Falcipain-2; Plasmodium falciparum; Molecular modelling|
|Academic Unit/Department:||Faculty of Science, Technology, Engineering and Mathematics (STEM) > Life, Health and Chemical Sciences
Faculty of Science, Technology, Engineering and Mathematics (STEM)
|Depositing User:||James Iley|
|Date Deposited:||21 Aug 2006|
|Last Modified:||02 Aug 2016 12:57|
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