Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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

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

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).

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

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Article Details

VOLUME: 6
ISSUE: 2
Year: 2009
Page: [139 - 145]
Pages: 7
DOI: 10.2174/157018009787582660
Price: $58