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- ISSN: 1570-1808
- E-ISSN: 1875-628X
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Presentation of the β -Carboxamidophosphonate Arrangement in Substrate Structures Targeting HIV-1 PR
- Source: Letters in Drug Design & Discovery, Volume 6, Issue 2, Mar 2009, p. 139 - 145
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- 01 Mar 2009
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).
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