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ID: ALA1139969
Journal: Bioorg Med Chem Lett
Title: Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.
Authors: Carroll WA, Kalvin DM, Perez Medrano A, Florjancic AS, Wang Y, Donnelly-Roberts DL, Namovic MT, Grayson G, Honoré P, Jarvis MF.
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 P2X(7) 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.
CiteXplore: 17482819