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1. Synthesis of Imidazo[1,2-a]pyridines as Antiviral Agents

Author

Mavel S, De Clercq E, Chavignon O, Graciela Andrei, Lhassani M, Alain Gueiffier, Robert Snoeck, Chapat Jp, Myriam Witvrouw, Teulade Jc, Elhakmaoui A, and Jan Balzarini

Subjects
Herpesvirus 3, Human, Imidazopyridine, Pyridines, Stereochemistry, viruses, Drug Evaluation, Preclinical, Cytomegalovirus, Antiviral Agents, Chemical synthesis, Virus, Cell Line, Inhibitory Concentration 50, Structure-Activity Relationship, chemistry.chemical_compound, Therapeutic index, Thioether, Chlorocebus aethiops, Drug Discovery, Side chain, Animals, Humans, Structure–activity relationship, Vero Cells, Bicyclic molecule, Imidazoles, virus diseases, chemistry, Molecular Medicine, HeLa Cells
Abstract

The synthesis of original imidazo[1,2-a]pyridines bearing a thioether side chain at the 3 position and their antiviral activity are reported. From the synthesized compounds, 4, 15, and 21 were highly active against human cytomegalovirus with a therapeutic index superior to 150. These compounds also showed pronounced activity against varicella-zoster virus. Their structure-activity relationship is discussed.

Published
1998
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2. Synthesis of acyclo-C-nucleosides in the imidazo[1,2-a]pyridine and pyrimidine series as antiviral agents

Author

Chapat Jp, J. C. Debouzy, Lhassani M, Robert Snoeck, Chavignon O, Teulade Jc, De Clercq E, Myriam Witvrouw, El Mokhtar Essassi, Graciela Andrei, Kerbal A, Elhakmaoui A, A. Gueiffier, Yves Blache, and Jan Balzarini

Subjects
Imidazopyridine, Pyrimidine, Stereochemistry, Pyridines, viruses, Chemical synthesis, Antiviral Agents, Virus, chemistry.chemical_compound, Structure-Activity Relationship, Drug Discovery, Pyridine, Chlorocebus aethiops, Tumor Cells, Cultured, Structure–activity relationship, Animals, Humans, Vero Cells, Bicyclic molecule, virus diseases, Nucleosides, Pyrimidines, chemistry, Molecular Medicine, Specific activity, HeLa Cells
Abstract

The synthesis and the antiviral activities of C-3 acyclic nucleoside analogues of imidazo[1,2-a]pyridine and pyrimidine are reported. From these compounds, 20, 21, 22, 23, 28, and 34 showed a specific activity against cytomegalovirus and/or varicella-zoster virus.

Published
1996

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