Methylene amine substituted arylindenopyrimidines as potent adenosine A sub(2A)/A sub(1) antagonists
A novel series of arylindenopyrimidines were identified as A sub(2A) and A sub(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 d...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-05, Vol.20 (9), p.2864-2867 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 20 |
| creator | 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 |
| description | A novel series of arylindenopyrimidines were identified as A sub(2A) and A sub(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. |
| doi_str_mv | 10.1016/j.bmcl.2010.03.042 |
| format | Article |
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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2010-05, Vol.20 (9), p.2864-2867 |
| issn | 0960-894X |
| language | eng |
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| source | Elsevier ScienceDirect Journals |
| title | Methylene amine substituted arylindenopyrimidines as potent adenosine A sub(2A)/A sub(1) antagonists |
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