Title of article
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists
Author/Authors
Patrick Betschmann، نويسنده , , Brian Bettencourt، نويسنده , , Diana Donnelly-Roberts، نويسنده , , Michael Friedman، نويسنده , , Jonathan George، نويسنده , , Gavin Hirst، نويسنده , , Nathan Josephsohn، نويسنده , , Donald Konopacki، نويسنده , , Biqin Li، نويسنده , , John Maull، نويسنده , , Michael J. Morytko، نويسنده , , Nigel StJohn Moore، نويسنده , , Marian Namovic، نويسنده , , Paul Rafferty، نويسنده , , Jose-Andres Salmeron-Garcia، نويسنده , , Edit Tarcsa، نويسنده , , Lu Wang، نويسنده , , Kevin Woller، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
3848
To page
3851
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
Antagonists , piperazine , Cyanoguanidine , P2X7
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799666
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