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Potent benzimidazolone based human beta(3)-adrenergic receptor agonists.

Finley, Don R; Bell, Michael G; Borel, Anthony G; Bloomquist, William E; Cohen, Marlene L; Heiman, Mark L; Kriauciunas, Aidas; Matthews, Donald P; Miles, Tania; Neel, David A; Rito, Christopher J; Sall, Daniel J; Shuker, Anthony J; Stephens, Thomas W; Tinsley, Frank C; Winter, Mark A; Jesudason, Cynthia D.

Bioorg Med Chem Lett ; 16(21): 5691-4, 2006 Nov 01.

Artículo en Inglés | MEDLINE | ID: mdl-16931005

RESUMEN

The synthesis and biological evaluation of a series of benzimidazolone beta(3) adrenergic receptor agonists are described. A trend toward the reduction of rat atrial tachycardia upon increasing steric bulk at the 3-position of the benzimidazolone moiety was observed.

Asunto(s)

Antagonistas de Receptores Adrenérgicos beta 3 , Agonistas Adrenérgicos beta/farmacología , Bencimidazoles/farmacología , Agonistas Adrenérgicos beta/química , Bencimidazoles/química , Humanos

3,3-Bisaryloxindoles as mineralocorticoid receptor antagonists.

Neel, David A; Brown, Matthew L; Lander, Peter A; Grese, Timothy A; Defauw, Jean M; Doti, Robert A; Fields, Todd; Kelley, Sally Ann; Smith, Stephon; Zimmerman, Karen M; Steinberg, Mitchell I; Jadhav, Prabhakar K.

Bioorg Med Chem Lett ; 15(10): 2553-7, 2005 May 16.

Artículo en Inglés | MEDLINE | ID: mdl-15863315

RESUMEN

Syntheses and SAR studies of 3,3-bisaryloxindole analogues provided potent mineralocorticoid receptor (MR) antagonists that were selective over other steroid nuclear hormone receptors.

Asunto(s)

Indoles/farmacología , Antagonistas de Receptores de Mineralocorticoides , Humanos , Ensayo de Unión Radioligante

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