Abuduaini T., Roy V., Marlet J., Gaudy-Graffin C., Brand D., Baronti Cécile, Touret F., Coutard B., McBrayer T. R., Schinazi R. F., Agrofoglio L. A. (2021). Synthesis and antiviral evaluation of (1,4-disubstituted-1,2,3-triazol)-(e)-2-methyl-but-2-Enyl nucleoside phosphonate prodrugs. Molecules, 26 (5), p. 1493 [18 p.].
Titre du document
Synthesis and antiviral evaluation of (1,4-disubstituted-1,2,3-triazol)-(e)-2-methyl-but-2-Enyl nucleoside phosphonate prodrugs
Année de publication
2021
Auteurs
Abuduaini T., Roy V., Marlet J., Gaudy-Graffin C., Brand D., Baronti Cécile, Touret F., Coutard B., McBrayer T. R., Schinazi R. F., Agrofoglio L. A.
Source
Molecules, 2021,
26 (5), p. 1493 [18 p.]
A series of hitherto unknown (1,4-disubstituted-1,2,3-triazol)-(E)-2-methyl-but-2-enyl nucleosides phosphonate prodrugs bearing 4-substituted-1,2,3-triazoles were prepared in a straight approach through an olefin acyclic cross metathesis as the key synthetic step. All novel compounds were evaluated for their antiviral activities against HBV, HIV and SARS-CoV-2. Among these molecules, only compound 15j, a hexadecyloxypropyl (HDP)/(isopropyloxycarbonyl-oxymethyl)-ester (POC) prodrug, showed activity against HBV in Huh7 cell cultures with 62% inhibition at 10 mu M, without significant cytotoxicity (IC50 = 66.4 mu M in HepG2 cells, IC50 = 43.1 mu M in HepG2 cells) at 10 mu M.
Plan de classement
Sciences fondamentales / Techniques d'analyse et de recherche [020]
;
Santé : généralités [050]
;
Entomologie médicale / Parasitologie / Virologie [052]
Localisation
Fonds IRD [F B010081107]
Identifiant IRD
fdi:010081107
