Presentation of the β-carboxamidophosphonate arrangement in substrate structures targeting HIV-1 PR

Author(s)
Author(s)
Wardle, N. J.
Hudson, H. R.
Matthews, R. W.
Nunn, C.
Vella, C.
Date Issued
2009
Publisher
Bentham Science
Journal
Letters in Drug Design & Discovery
Volume
6
Issue
2
Start page
139
End page
145
Abstract
Novel O,O-diethyl 1-benzamido-2,2-biscarbamoylethanephosphonates were synthesised as putative substrates to HIV-1 PR, to exploit the state of activation of the phosphonate electrophilic function in β-carboxamidophosphonate arrangements. O,O-Diethyl 1-benzamido-2,2-bis[(1S)-N-(1-benzyl-2-hydroxyethyl)carbamoyl]ethanephosphonate exhibited moderate anti-HIV activity in vitro (EC50 = 53 μrbamoyl]ethanephosphonate inhibited HIV-1 PR (IC50 = 31 μM).
URI
DOI
SFU Affiliated Publication
No
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