Peptide-nucleoside conjugates: Synthesis and anti-HIV activities

Article abstract of DOI:10.1080/15257779508010699

New peptide-nucleosides which consist of an anti-RT nucleoside and anti- protease peptide moieties, were designed in order to investigate their anti- HIV-1 properties. The synthesis of these new analogues was achieved using BOP coupling reagent which avoided the protection and deprotection steps of the 5'-OH group of the nucleoside part. These new compounds tested on MT₄ infected cells show no increase in anti-HIV activities compared to that of the component pieces. Interestingly we found that the 5'-(tert- butyldiphenyl)silyl analogues show anti-HIV activities equivalent to that of the 5'-free OH corresponding compounds. This result suggests a possible interaction of these compounds at a non-substrate binding site of the reverse transcriptase.

Full text of DOI:10.1080/15257779508010699

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Nucleosides and Nucleotides
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Peptide-Nucleoside Conjugates:
Synthesis and Anti-HIV Activities
Nicolas Mourier a b , Carole Trabaud a b , Jean Christophe Graciet
a b , Vanessa Simon a b , Valérie Niddam a b , Philippe Faury a
b , Anne Sophie Charvet a b , Michel Camplo a b , Jean-Claude
Chermann b & Jean Louis Kraus a b
a Laboratoire de Chimie Biomoléculaire, Faculté des Sciences de
Luminy, case 901 13288, MARSEILLE CEDEX, 9, FRANCE Phone:
91.26.91.41 Fax: 91.26.91.41
b INSERM Unité U-322, Unité des Rétrovirus et Maladies
Associées, Campus universitaire de Luminy, BP 33, 13273,
MARSEILLE CEDEX, 9, FRANCE Phone: 91.82.75.41.
Version of record first published: 24 Sep 2006.
To cite this article: Nicolas Mourier , Carole Trabaud , Jean Christophe Graciet , Vanessa Simon ,
Valérie Niddam , Philippe Faury , Anne Sophie Charvet , Michel Camplo , Jean-Claude Chermann
& Jean Louis Kraus (1995): Peptide-Nucleoside Conjugates: Synthesis and Anti-HIV Activities,
Nucleosides and Nucleotides, 14:6, 1393-1402
To link to this article: http://dx.doi.org/10.1080/15257779508010699
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