ganciclovir and Herpes-Zoster

The synthesis of original imidazo[1,2-a]pyridines bearing a thioether side chain at the 3 position and diversely substituted on the 6 or 8 position, and their antiviral activities are reported. From the synthesized compounds, the imidazo[1,2-a]pyridines bearing a 5 membered heterocycle (thiophene, furane or pyrrole) in the 6 position or a phenylthio group in the 6 or 8 position were the most potent against human cytomegalovirus (CMV) and varicella-zoster virus (VZV), whereas several other congeners, while less potent, were more selective in their inhibitory activity against VZV and CMV. These compounds showed similar activity against thymidine kinase competent (TK+) and deficient (TK-) VZV strains, demonstrating a mechanism of action independent of the viral thymidine kinase.

Topics: Antiviral Agents; Cell Survival; Cells, Cultured; Cytomegalovirus; Cytomegalovirus Infections; Herpes Zoster; Herpesvirus 3, Human; Humans; Imidazoles; Lung; Molecular Structure; Pyridines; Structure-Activity Relationship

A novel series of 2-aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxamides have been identified as potent antivirals against human herpesviruses. These compounds demonstrate broad-spectrum inhibition of the herpesvirus polymerases HCMV, HSV-1, EBV, and VZV with high specificity compared to human DNA polymerases.

Topics: Antiviral Agents; Binding, Competitive; Cytomegalovirus; DNA-Directed DNA Polymerase; Enzyme Inhibitors; Ethylamines; Exodeoxyribonucleases; Herpes Zoster; Herpesviridae; Herpesvirus 1, Human; Herpesvirus 4, Human; Humans; Models, Chemical; Nucleic Acid Synthesis Inhibitors; Pyridines; Structure-Activity Relationship; Viral Proteins