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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and S.W. A. Bligh

Volume 6, Issue 2, 2009

Page: [139 - 145] Pages: 7

DOI: 10.2174/157018009787582660

Price: $65

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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