| Title : Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists - Betschmann_2008_Bioorg.Med.Chem.Lett_18_3848 |
| Author(s) : 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 |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :3848 , 2008 |
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Abstract :
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. |
| PubMedSearch : Betschmann_2008_Bioorg.Med.Chem.Lett_18_3848 |
| PubMedID: 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 (2008)
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists
Bioorganic & Medicinal Chemistry Lett
18 :3848
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 (2008)
Bioorganic & Medicinal Chemistry Lett
18 :3848