Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists

Alexander Alanine; Lilli Anselm; Lucinda Steward; Stefan Thomi; Walter Vifian; Michael D Groaning

doi:10.1016/j.bmcl.2003.09.095

Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists

Bioorg Med Chem Lett. 2004 Feb 9;14(3):817-21. doi: 10.1016/j.bmcl.2003.09.095.

Authors

Alexander Alanine¹, Lilli Anselm, Lucinda Steward, Stefan Thomi, Walter Vifian, Michael D Groaning

Affiliation

¹ F Hoffmann-La Roche AG, Pharmaceuticals Division, Discovery Chemistry, Lead Generation, Basel CH 4070, Switzerland.

PMID: 14741297
DOI: 10.1016/j.bmcl.2003.09.095

Abstract

The synthesis and in vitro structure-activity relationships (SAR) of a series of triazoles as A(2A) receptor antagonists is reported. This resulted in the identification of potent, selective and permeable 1,2,4-triazoles such as 42 for further optimization and evaluation in vivo.

MeSH terms

Adenosine A2 Receptor Antagonists*
Animals
Cell Membrane / chemistry*
In Vitro Techniques
Molecular Structure
Rats
Structure-Activity Relationship
Triazoles / chemical synthesis*
Triazoles / pharmacology*

Substances

Adenosine A2 Receptor Antagonists
Triazoles
1,2,4-triazole