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Bioorg Med Chem Lett. 2008 Mar 15;18(6):1778-83. doi: 10.1016/j.bmcl.2008.02.032. Epub 2008 Feb 16.

Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.

Author information

1
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.

PMID:
18329269
DOI:
10.1016/j.bmcl.2008.02.032
[Indexed for MEDLINE]

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