Bioorganic and Medicinal Chemistry Letters p. 1778 - 1783 (2008)
Update date:2022-08-04
Topics: Purification and characterization N-Substitution Synthesis of the Pyrimidine Ring Introduction of the Phenoxyacetamide Group
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, Maria I.
Prat, Maria
Gual, Silvia
Diaz, Jose-Luis
Saunders, John
Slee, Deborah H.
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
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