کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1364957 | 981550 | 2008 | 4 صفحه PDF | دانلود رایگان |
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.
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.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 14, 15 July 2008, Pages 3848–3851