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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology
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Cell Line
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Chlorocebus aethiops
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Cytomegalovirus / drug effects
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Drug Evaluation, Preclinical
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HeLa Cells
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Herpesvirus 3, Human / drug effects
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology
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Inhibitory Concentration 50
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Structure-Activity Relationship
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Vero Cells
Substances
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2-methyl-3-((phenylethyl)thiomethyl)imidazo(1,2-a)pyridine
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6-bromo-8-methyl-3-((phenylethyl)thiomethyl)imidazo(1,2-a)pyridine
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7-methyl-3-((phenylethyl)thiomethyl)imidazo(1,2-a)pyridine
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Antiviral Agents
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Imidazoles
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Pyridines