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Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists |
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| Authors: | Zhang Xiaohu Rueter Jaimie K Chen Yongsheng Moorjani Manisha Lanier Marion C Lin Emily Gross Raymond S Tellew John E Williams John P Lechner Sandra M Markison Stacy Joswig Tanya Malany Siobhan Santos Mark Castro-Palomino Julio C Crespo María I Prat Maria Gual Silvia Díaz José-Luis Saunders John Slee Deborah H |
| Affiliation: | Department of Medicinal Chemistry, Neurocrine Biosciences, 12790 El Camino Real, San Diego, CA 92130, USA. litiger_99@yahoo.com |
| Abstract: | A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A(2A) antagonists is described. SAR studies led to compound 14 with excellent potency (K(i) = 0.4 nM), selectivity (A(1)/A(2A) > 100), and efficacy (MED 10 mg/kg p.o.) in the rat haloperidol-induced catalepsy model for Parkinson's disease. |
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