Presentation of the β -Carboxamidophosphonate Arrangement in Substrate Structures Targeting HIV-1 PR

Title: Presentation of the β -Carboxamidophosphonate Arrangement in Substrate Structures Targeting HIV-1 PR

Volume: 6 Issue: 2

Author(s): N. J. Wardle, H. R. Hudson, R. W. Matthews, C. Nunn, C. Vella and S.W. A. Bligh

Affiliation:

Keywords: β-carboxamidophosphonates, HIV-1 PR inhibitors, Anti-HIV agents

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).

Cite this article as:

Wardle J. N., Hudson R. H., Matthews W. R., Nunn C., Vella C. and Bligh A. S.W., Presentation of the β -Carboxamidophosphonate Arrangement in Substrate Structures Targeting HIV-1 PR, Letters in Drug Design & Discovery 2009; 6 (2) . https://dx.doi.org/10.2174/157018009787582660