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Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists.
Dyatkin, Alexey B; Gong, Yong; Miskowski, Tamara A; Kimball, Edward S; Prouty, Stephen M; Fisher, M Carolyn; Santulli, Rosemary J; Schneider, Craig R; Wallace, Nathaniel H; Hornby, Pamela J; Diamond, Craig; Kinney, William A; Maryanoff, Bruce E; Damiano, Bruce P; He, Wei.
Afiliación
  • Dyatkin AB; Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, LLC., Spring House, PA 19477-0776, USA. adyatkin@prdus.jnj.com
Bioorg Med Chem ; 13(24): 6693-702, 2005 Dec 15.
Article en En | MEDLINE | ID: mdl-16112583
A series of N-carboxy, N-alkyl, and N-carboxamido azabicyclo[2.2.2]octane carboxamides were prepared and assayed for inhibition of alpha4beta1-VCAM-1 and alpha4beta7-MAdCAM-1 interactions. Potency and alpha4beta1/alpha4beta7 selectivity were sensitive to the substituent R1-R3 in the structures 6, 7, and 8. Several compounds demonstrated low nanomolar balanced alpha4beta1/alpha4beta7 in vitro activity. Two compounds were selected for in vivo leukocytosis studies and demonstrated increases in circulating lymphocytes up to 250% over control.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos Aza / Integrinas / Integrina alfa4beta1 / Aminoácidos Cíclicos Límite: Animals Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2005 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Buscar en Google
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos Aza / Integrinas / Integrina alfa4beta1 / Aminoácidos Cíclicos Límite: Animals Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2005 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido