Structure–affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A 2A receptor

…, Z Li, Z Gao, S Meyer, B Blackburn, JA Zablocki

Index: Palle, Venkata P.; Elzein, Elfatih O.; Gothe, Scott A.; Li, Zhihe; Gao, Zhenhai; Meyer, Stephanie; Blackburn, Brent; Zablocki, Jeff A. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 20 p. 2935 - 2939

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Citation Number: 22

Abstract

The structure–affinity relationships of two novel 2-substituted adenosine series containing a substituted pyrazole attached at the N-1 or C-4 position for the adenosine (ADO) A2A receptor are described. Compounds in the 2-(N-1-pyrazolyl) adenosine series IV provided the highest affinity for the ADO A2A receptor as compared to the 2-(C-4-pyrazolyl) series V. The main structural differences between the two series point to the N-1 nitrogen of series ...