Synthesis of imidazo[1,2-a]pyridine derivatives as antiviral agents.
The synthesis and antiviral activity of original dibromoimidazo[1,2-a]pyridines bearing a thioether side chain are reported. Molecular modeling was used to identify biophoric structural patterns that are common to 16 compounds. Structure-activity relationship (SAR) studies identified hydrophobicity (logP) as the most important factor for activity. From these SAR studies, the antiviral activity could be predicted.
Mavel
S
S
Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, Tours, France.
Renou
J L
JL
Galtier
C
C
Snoeck
R
R
Andrei
G
G
Balzarini
J
J
De Clercq
E
E
Gueiffier
A
A
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D015726:Giant Cells / Q000187:drug effects / Q000821:virology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D008968:Molecular Conformation; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D021281:Quantitative Structure-Activity Relationship
D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D000998:Antiviral Agents; D007093:Imidazoles; D011725:Pyridines