Title of article :
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists
Author/Authors :
William A. Carroll، نويسنده , , Douglas M. Kalvin، نويسنده , , Arturo Perez-Medrano، نويسنده , , Alan S. Florjancic، نويسنده , , Ying Wang، نويسنده , , Diana L. Donnelly-Roberts، نويسنده , , Marian T. Namovic، نويسنده , , George Grayson، نويسنده , , Prisca Honore، نويسنده , , Michael F. Jarvis، نويسنده ,
Abstract :
Structure–activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated and the pendant benzyl substitution was reoptimized with a triazole isostere. Triazole-based P2X7 antagonists were identified with similar potency to the lead compound 4 but with improved physiochemical properties. Compound 12 was active in a rat model of neuropathic pain.
