Presentation of the β -Carboxamidophosphonate Arrangement in Substrate Structures Targeting HIV-1 PR
N. J. Wardle,
H. R. Hudson,
R. W. Matthews,
S.W. A. Bligh.
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).
Keywords: β-carboxamidophosphonates, HIV-1 PR inhibitors, Anti-HIV agents
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