Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

Shook, Brian C; Rassnick, Stefanie; Hall, Daniel; Rupert, Kenneth C; Heintzelman, Geoffrey R; Hansen, Kristen; Chakravarty, Devraj; Bullington, James L; Scannevin, Robert H; Magliaro, Brian; Westover, Lori; Carroll, Karen; Lampron, Lisa; Russell, Ronald; Branum, Shawn; Wells, Kenneth; Damon, Sandra; Youells, Scott; Li, Xun; Osbourne, Mel; Demarest, Keith; Tang, Yuting; Rhodes, Kenneth; Jackson, Paul F

Shook, Brian C; Rassnick, Stefanie; Hall, Daniel; Rupert, Kenneth C; Heintzelman, Geoffrey R; Hansen, Kristen; Chakravarty, Devraj; Bullington, James L; Scannevin, Robert H; Magliaro, Brian; Westover, Lori; Carroll, Karen; Lampron, Lisa; Russell, Ronald; Branum, Shawn; Wells, Kenneth; Damon, Sandra; Youells, Scott; Li, Xun; Osbourne, Mel; Demarest, Keith; Tang, Yuting; Rhodes, Kenneth; Jackson, Paul F.

Afiliación

Shook BC; Johnson & Johnson Pharmaceutical Research and Development, L.L.C., Welsh and McKean Roads, PO Box 776, Spring House, PA 19477, United States. bshook@its.jnj.com

Bioorg Med Chem Lett ; 20(9): 2864-7, 2010 May 01.

Article en En | MEDLINE | ID: mdl-20347304

ABSTRACT

ABSTRACT

A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent activity in mouse models of Parkinson's disease when dosed orally.

Asunto(s)

Antagonistas del Receptor de Adenosina A1; Antagonistas del Receptor de Adenosina A2; Aminas/química; Neurotransmisores/química; Pirimidinas/química; Aminas/síntesis química; Aminas/uso terapéutico; Animales; Catalepsia/tratamiento farmacológico; Modelos Animales de Enfermedad; Ratones; Neurotransmisores/síntesis química; Neurotransmisores/uso terapéutico; Pirimidinas/síntesis química; Pirimidinas/uso terapéutico; Receptor de Adenosina A1/metabolismo; Receptor de Adenosina A2A/metabolismo; Relación Estructura-Actividad

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Neurotransmisores / Antagonistas del Receptor de Adenosina A1 / Antagonistas del Receptor de Adenosina A2 / Aminas Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2010 Tipo del documento: Article País de afiliación: Estados Unidos

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