| 18595695 |
Betschmann P, Bettencourt B, Donnelly-Roberts D, Friedman M, George J, Hirst G, Josephsohn N, Konopacki D, Li B, Maull J, Morytko MJ, Moore NS, Namovic M, Rafferty P, Salmeron-Garcia JA, Tarcsa E, Wang L, Woller K: Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists. . Bioorg Med Chem Lett. 2008 Jul 15;18(14):3848-51. Epub 2008 Jun 20.
A novel series of cyanoguanidine-piperazine P2X (7) antagonists were identified and structure-activity relationship (SAR) studies described. Compounds were assayed for activity at human and rat P2X (7) receptors in addition to their ability to inhibit IL-1 beta release from stimulated human whole blood cultures. Compound 27 possesses potent activity (0.12 microM) in this latter assay and demonstrates moderate clearance in-vivo. |
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