Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.

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Palle VP, Elzein EO, Gothe SA, Li Z, Gao Z, Meyer S, Blackburn B, Zablocki JA

Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2935-9.

PubMed ID

12270178 [ View in PubMed

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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 IV imparting more favorable binding interactions with the receptor than those of series V.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Regadenoson	Adenosine receptor A2a	Ki (nM)	1269000	N/A	N/A	Details
Regadenoson	Adenosine receptor A2a	Ki (nM)	1120	N/A	N/A	Details