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Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists |
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| Authors: | Carroll William A Kalvin Douglas M Perez Medrano Arturo Florjancic Alan S Wang Ying Donnelly-Roberts Diana L Namovic Marian T Grayson George Honoré Prisca Jarvis Michael F |
| Affiliation: | Abbott Laboratories, Neuroscience Research, 100 Abbott Park Road, Abbott Park, IL 60064, USA. william.a.carroll@abbott.com |
| 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. |
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