Synthesis and SAR Evaluation of 1,2,4-Triazoles as A2A Receptor Antagonists.

Abstract The synthesis and in vitro structure–activity relationships (SAR) of a series of triazoles as A2A 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.