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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.
Afiliação
  • 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 em En | MEDLINE | ID: mdl-20347304
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Neurotransmissores / Antagonistas do Receptor A1 de Adenosina / Antagonistas do Receptor A2 de Adenosina / Aminas Limite: Animals Idioma: En Ano de publicação: 2010 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Neurotransmissores / Antagonistas do Receptor A1 de Adenosina / Antagonistas do Receptor A2 de Adenosina / Aminas Limite: Animals Idioma: En Ano de publicação: 2010 Tipo de documento: Article