Synthesis and antiviral activity of 2'-deoxy-4'-thio purine nucleosides.
J Med Chem
; 39(2): 538-42, 1996 Jan 19.
Article
de En
| MEDLINE
| ID: mdl-8558524
ABSTRACT
A series of 2'-deoxy-4'-thioribo purine nucleosides was prepared by trans-N-deoxyribosylase-catalyzed reaction of 2'-deoxy-4'-thiouridine with a variety of purine bases. This synthetic procedure is an improvement over methods previously used to prepare purine 4'-thio nucleosides. The compounds were tested against hepatitis B virus (HBV), human cytomegalovirus (HCMV), herpes simplex virus (HSV-1 and HSV-2), varicella zoster virus (VZV), and human immunodeficiency virus (HIV-1). Cytotoxicity was determined in a number of cell lines. Several compounds were extremely potent against HBV and HCMV and had moderate to severe cytotoxicity in vitro. The lead compound from the series, 2-amino-6-(cyclopropylamino)purine 2'-deoxy-4'-thioriboside, was the most potent and selective agent against HCMV and HBV replication in vitro; however, this analogue was nephrotoxic when tested in vivo.
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Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Antiviraux
/
Nucléoside purique
Limites:
Humans
Langue:
En
Journal:
J Med Chem
Sujet du journal:
QUIMICA
Année:
1996
Type de document:
Article
Pays d'affiliation:
États-Unis d'Amérique