6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists

Eugenia Kiselgof; Deen B Tulshian; Leyla Arik; Hongtao Zhang; Ahmad Fawzi

doi:10.1016/j.bmcl.2005.02.031

6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists

Bioorg Med Chem Lett. 2005 Apr 15;15(8):2119-22. doi: 10.1016/j.bmcl.2005.02.031.

Authors

Eugenia Kiselgof¹, Deen B Tulshian, Leyla Arik, Hongtao Zhang, Ahmad Fawzi

Affiliation

¹ Schering-Plough Research Institute, Chemical Research, 2015 Galloping Hill Road, MS 2545, Kenilworth, NJ 07033, USA.

PMID: 15808481
DOI: 10.1016/j.bmcl.2005.02.031

Abstract

Structure-activity relationships have been investigated through substitutions at the 9-position of the 2-amino-6-(2-furanyl) purine (5) to identify novel and selective A(2A) adenosine receptor antagonists. Several potent and selective antagonists were identified. In particular, compounds 20, 25, and 26 show very high affinity with excellent selectivity.

MeSH terms

Adenosine A2 Receptor Antagonists*
Cell Line
Humans
Protein Binding / drug effects
Protein Binding / physiology
Pyrimidines / chemistry*
Pyrimidines / metabolism
Pyrimidines / pharmacology*
Receptor, Adenosine A2A / metabolism
Receptor, Adenosine A2A / physiology
Triazoles / chemistry*
Triazoles / metabolism
Triazoles / pharmacology*

Substances

5-amino-7-(2-phenylethyl)-2-(2-furyl)pyrazolo(4,3-e)-1,2,4-triazolo(1,5-c)pyrimidine
Adenosine A2 Receptor Antagonists
Pyrimidines
Receptor, Adenosine A2A
Triazoles