Aza-bicyclic amino acid sulfonamides as α4β 14β7 integrin antagonists

Alexey B. Dyatkin, William J. Hoekstra, William A. Kinney, Maria Kontoyianni, Rosemary J. Santulli, Edward S. Kimball, M. Carolyn Fisher, Stephen M. Prouty, William M. Abraham, Patricia Andrade-Gordon, Dennis J. Hlasta, Wei He, Pamela J. Hornby, Bruce P. Damiano, Bruce E. Maryanoff

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


The design, synthesis, and biological activity of novel α 4β1 and α4β7 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 α 4β1-selective and dual α4β 14β7 antagonists. Potent compounds 11i, 11h, and 14 were effective in the antigen-sensitized sheep model of asthma.

Original languageEnglish (US)
Pages (from-to)591-596
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number3
StatePublished - Feb 9 2004

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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