| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376780 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A2A antagonists is described. SAR studies led to compound 14 with excellent potency (Ki = 0.4 nM), selectivity (A1/A2A > 100), and efficacy (MED 10 mg/kg po) in the rat haloperidol-induced catalepsy model for Parkinson’s disease.
Graphical abstractA series of N-pyrimidinyl-2-phenoxyacetamide adenosine A2A antagonists is described. SAR studies led to compound 14 with excellent potency, selectivity, and efficacy in the rat haloperidol-induced catalepsy model for Parkinson’s disease.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Xiaohu Zhang, Jaimie K. Rueter, Yongsheng Chen, Manisha Moorjani, Marion C. Lanier, Emily Lin, Raymond S. Gross, John E. Tellew, John P. Williams, Sandra M. Lechner, Stacy Markison, Tanya Joswig, Siobhan Malany, Mark Santos, Julio C. Castro-Palomino,