Bioorganic and Medicinal Chemistry Letters p. 591 - 596 (2004)
Update date:2022-08-04
Topics: Aza-bicyclic Amino Acid Sulfonamides α4β1/α4β7 Integrin Antagonists
Dyatkin, Alexey B.
Hoekstra, William J.
Kinney, William A.
Kontoyianni, Maria
Santulli, Rosemary J.
Kimball, Edward S.
Fisher, M. Carolyn
Prouty, Stephen M.
Abraham, William M.
Andrade-Gordon, Patricia
Hlasta, Dennis J.
He, Wei
Hornby, Pamela J.
Damiano, Bruce P.
Maryanoff, Bruce E.
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 1/α4β7 antagonists. Potent compounds 11i, 11h, and 14 were effective in the antigen-sensitized sheep model of asthma. 2003 Elsevier Science Ltd. All rights reserved.
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