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Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists |
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| Authors: | Morytko Michael J Betschmann Patrick Woller Kevin Ericsson Anna Chen Haipeng Donnelly-Roberts Diana L Namovic Marian T Jarvis Michael F Carroll William A Rafferty Paul |
| Affiliation: | Abbott Bioresearch Center, Department of Medicinal Chemistry, 381 Plantation Street, Worcester, MA 01605, USA. |
| Abstract: | A novel series of cyanoguanidine-piperazine P2X(7) antagonists was designed based upon the structure of A-740003. Structure-activity relationship (SAR) studies focused on the piperazine moiety and the right hand side substitution. Compounds were assayed for activity at human and rat P2X(7) receptors and compound 29 was found to possess potent activity (IC(50)=30-60 nM) at both species. |
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