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

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

Affiliation

  • 1 Department of Bioorganic Chemistry, CV Therapeutics, 3172 Porter Drive, Palo Alto, CA 94304, USA. jeff.zablocki@cut.com
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.

Figures
Products