Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin.

Matthews, Jay M; Liotta, Fina; Hageman, William; Rivero, Ralph A; Westover, Lori; Yang, Maria; Xu, Jun; Demarest, Keith

Matthews, Jay M; Liotta, Fina; Hageman, William; Rivero, Ralph A; Westover, Lori; Yang, Maria; Xu, Jun; Demarest, Keith.

Afiliación

Matthews JM; Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, Spring House, PA 19477-0776, USA. jmatthew@pruis.jnj.com

Bioorg Med Chem Lett ; 14(5): 1155-9, 2004 Mar 08.

Article en En | MEDLINE | ID: mdl-14980655

RESUMEN

The use of a multiplex mimetic assay led us to identify 1,4-dihydropyrimidines with potent and selective calcitonin receptor mimetic activity. Subsequent modification of the dihydropyrimidine scaffold led to a series of molecules that were efficacious in a neonatal mouse calvaria in vitro model. Dihydropyrimidine 5h, in particular, was identified as a calcitonin mimetic (EC(50)=6 microM), active in-vivo in the Weanling rat model when administered subcutaneously.

Asunto(s)

Calcitonina/química; Calcitonina/fisiología; Dihidropiridinas/química; Imitación Molecular/fisiología; Pirimidinas/química; Animales; Calcitonina/orina; Línea Celular; Dihidropiridinas/farmacología; Dihidropiridinas/orina; Humanos; Pirimidinas/farmacología; Pirimidinas/orina; Ratas

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Calcitonina / Dihidropiridinas / Imitación Molecular Límite: Animals / Humans 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

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