Peer-reviewed veterinary case report
Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2004
- Authors:
- Dyatkin, Alexey B et al.
- Affiliation:
- Drug Discovery · United States
Abstract
The design, synthesis, and biological activity of novel alpha(4)beta(1) and alpha(4)beta(7) integrin antagonists, containing a bridged azabicyclic nucleus, are reported. Conformational analysis of targets containing an azabicyclo[2.2.2]octane carboxylic acid and known integrin antagonists indicated that this azabicycle would be a suitable molecular scaffold. Variation of substituents on the pendant arylsulfonamide and phenylalanine groups resulted in potent alpha(4)beta(1)-selective and dual alpha(4)beta(1)/alpha(4)beta(7) antagonists. Potent compounds 11i, 11h, and 14 were effective in the antigen-sensitized sheep model of asthma.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/14741249/