Literature DB >> 10498207

Simple mono-derivatisation of the aryl moiety of D4A and DDA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture.

A Q Siddiqui1, C McGuigan, C Ballatore, O Wedgwood, E De Clercq, J Balzarini.   

Abstract

Simple mono-derivatisation of the aryl moiety of some phosphoramidate pronucleotide derivatives of d4A and ddA served to increase the lipophilicity of these membrane-soluble prodrugs. A concomitant and significant enhancement of potency against HIV-1 and HIV-2 in vitro was observed for the ddA- and d4A-based prodrugs compared to the original underivatised prodrugs.

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Year:  1999        PMID： 10498207     DOI： 10.1016/s0960-894x(99)00416-3

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Synthesis of nucleoside phosphate and phosphonate prodrugs.

Authors:  Ugo Pradere; Ethel C Garnier-Amblard; Steven J Coats; Franck Amblard; Raymond F Schinazi
Journal:  Chem Rev       Date:  2014-08-21       Impact factor: 60.622

2.  Enhanced inhibition of the EDHF phenomenon by a phenyl methoxyalaninyl phosphoramidate derivative of dideoxyadenosine.

Authors:  Tudor M Griffith; Andrew T Chaytor; David H Edwards; Felice Daverio; Christopher McGuigan
Journal:  Br J Pharmacol       Date:  2004-05       Impact factor: 8.739

Review 3.  Phosphoramidates and phosphonamidates (ProTides) with antiviral activity.

Authors:  Magdalena Slusarczyk; Michaela Serpi; Fabrizio Pertusati
Journal:  Antivir Chem Chemother       Date:  2018 Jan-Dec
  3 in total

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