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. doi: 10.1016/s0960-894x(02)00609-1.
Venkata P Palle  1 ,  Elfatih O Elzein ,  Scott A Gothe ,  Zhihe Li ,  Zhenhai Gao ,  Stephanie Meyer ,  Brent Blackburn ,  Jeff A Zablocki
Affiliations
  • 1. Department of Bioorganic Chemistry, CV Therapeutics, 3172 Porter Drive, Palo Alto, CA 94304, USA. [email protected]
PMID: 12270178 DOI: 10.1016/s0960-894x(02)00609-1
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.

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