Synthesis and Activity of N-cyanoguanidine-piperazine P2X7 Antagonists.

Patrick Betschmann,Brian Bettencourt,Diana Donnelly-Roberts,Michael Friedman,Jonathan George,Gavin Hirst,Nathan Josephsohn,Donald Konopacki,Biqin Li,John Maull,Michael J. Morytko,Nigel StJohn Moore,Marian Namovic,Paul Rafferty, Jose-Andres Salmeron-Garcia,Edit Tarcsa,Lu Wang,Kevin Woller

Bioorganic & medicinal chemistry letters（2008）

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摘要

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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关键词

P2X7,antagonists,cyanoguanidine,piperazine

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