Abstract
Analogs of (E)-5-(2-bromovinyl)-2'-deoxycytidine (BrVdCyd) (1) by substitution at N(4) were synthesized to impart resistance against deamination. The anti-HSV-1 activity and solution conformation of these analogs were determined. N(4)-Acetyl-BrVdCyd (2) was a potent inhibitor of HSV-1 replication whereas N(4)-propanoyl-BrVdCyd (3) had good activity and N(4)-Butanoyl-BrVdCyd (4) had only low activity against HSV-1 replication. N(4)-Methyl-BrVdCyd (5) was devoid of activity against HSV-1.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antiviral Agents / chemical synthesis
-
Antiviral Agents / chemistry*
-
Antiviral Agents / pharmacology*
-
Bromodeoxycytidine / analogs & derivatives*
-
Bromodeoxycytidine / chemistry
-
Bromodeoxycytidine / pharmacology
-
Carbohydrate Conformation
-
Cell Line
-
Drug Stability
-
Humans
-
Microbial Sensitivity Tests
-
Simplexvirus / drug effects*
-
Virus Replication / drug effects
Substances
-
Antiviral Agents
-
Bromodeoxycytidine
-
5-(2-bromovinyl)-2'-deoxycytidine