Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists

Abstract A novel series of aminotriazole-based P2X 7 antagonists was synthesized, and their structure–activity relationships (SAR) were investigated for activity at both human and rat P2X 7 receptors. Most compounds showed greater potency at the human receptor although several analogs were discovered with potent activity (pIC 50  ⩾ 7.5) at both human and rat P2X 7 .