Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 14, Pages 3848-3851Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.06.055
Keywords
P2X7; antagonists; cyanoguanidine; piperazine
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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 mu M) in this latter assay and demonstrates moderate clearance in-vivo. (C) 2008 Elsevier Ltd. All rights reserved.
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