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Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
Dyatkin, Alexey B; Hoekstra, William J; Kinney, William A; Kontoyianni, Maria; Santulli, Rosemary J; Kimball, Edward S; Fisher, M Carolyn; Carolyn Fisher, M; Prouty, Stephen M; Abraham, William M; de Garavilla, Lawrence; Andrade-Gordon, Patricia; Hlasta, Dennis J; He, Wei; Hornby, Pamela J; Damiano, Bruce P; Maryanoff, Bruce E.
Afiliación
  • Dyatkin AB; Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, LLC, Spring House, PA 19477-0776, USA. adyatkin@prdus.jnj.com
Bioorg Med Chem Lett ; 14(3): 591-6, 2004 Feb 09.
Article en En | MEDLINE | ID: mdl-14741249
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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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Sulfonamidas / Compuestos Aza / Integrinas / Integrina alfa4beta1 / Antígenos Helmínticos Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2004 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Buscar en Google
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PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Sulfonamidas / Compuestos Aza / Integrinas / Integrina alfa4beta1 / Antígenos Helmínticos Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2004 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido