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

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 w...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-05, Vol.20 (9), p.2864-2867
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine A1 Receptor Antagonists Adenosine A2 Receptor Antagonists Amines - chemical synthesis Amines - chemistry Amines - therapeutic use Animals Catalepsy - drug therapy Disease Models, Animal Mice Neurotransmitter Agents - chemical synthesis Neurotransmitter Agents - chemistry Neurotransmitter Agents - therapeutic use Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - therapeutic use Receptor, Adenosine A1 - metabolism Receptor, Adenosine A2A - metabolism Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2010.03.042