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Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists |
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| Authors: | Betschmann Patrick Bettencourt Brian Donnelly-Roberts Diana Friedman Michael George Jonathan Hirst Gavin Josephsohn Nathan Konopacki Donald Li Biqin Maull John Morytko Michael J Moore Nigel Stjohn Namovic Marian Rafferty Paul Salmeron-Garcia Jose-Andres Tarcsa Edit Wang Lu Woller Kevin |
| Affiliation: | aAbbott Bioresearch Center, Department of Medicinal Chemistry, 381 Plantation Street, Worcester, MA 01605, USA |
| Abstract: | A novel series of cyanoguanidine-piperazine P2X7 antagonists were identified and structure–activity relationship (SAR) studies described. Compounds were assayed for activity at human and rat P2X7 receptors in addition to their ability to inhibit IL-1β release from stimulated human whole blood cultures. Compound 27 possesses potent activity (0.12 μM) in this latter assay and demonstrates moderate clearance in-vivo. |
| Keywords: | P2X7 Antagonists Cyanoguanidine Piperazine |
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