Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.

Henke, B R; Adkison, K K; Blanchard, S G; Leesnitzer, L M; Mook, R A; Plunket, K D; Ray, J A; Roberson, C; Unwalla, R; Willson, T M

Henke, B R; Adkison, K K; Blanchard, S G; Leesnitzer, L M; Mook, R A; Plunket, K D; Ray, J A; Roberson, C; Unwalla, R; Willson, T M.

Afiliación

Henke BR; Department of Medicinal Chemistry, Glaxo Wellcome Research and Development, Research Triangle Park, NC 27709, USA.

Bioorg Med Chem Lett ; 9(23): 3329-34, 1999 Dec 06.

Article en En | MEDLINE | ID: mdl-10612594

RESUMEN

The synthesis and structure-activity relationships of a novel series of indole 5-carboxylic acids that bind and activate peroxisome proliferator-activated receptor gamma (PPARgamma) are reported. These new analogs are selective for PPARgamma vs the other PPAR subtypes, and the most potent compounds in this series are comparable to in vitro potencies at PPARgamma reported for the thiazolidinedione-based antidiabetic drugs currently in clinical use.

Asunto(s)

Indoles/síntesis química; Indoles/farmacología; Receptores Citoplasmáticos y Nucleares/agonistas; Factores de Transcripción/agonistas; Animales; Disponibilidad Biológica; Humanos; Indoles/farmacocinética; Ratas; Relación Estructura-Actividad

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Factores de Transcripción / Receptores Citoplasmáticos y Nucleares / Indoles Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 1999 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido

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