1001183-82-9Relevant academic research and scientific papers
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists
Betschmann, Patrick,Bettencourt, Brian,Donnelly-Roberts, Diana,Friedman, Michael,George, Jonathan,Hirst, Gavin,Josephsohn, Nathan,Konopacki, Donald,Li, Biqin,Maull, John,Morytko, Michael J.,Moore, Nigel StJohn,Namovic, Marian,Rafferty, Paul,Salmeron-Garcia, Jose-Andres,Tarcsa, Edit,Wang, Lu,Woller, Kevin
scheme or table, p. 3848 - 3851 (2009/04/10)
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.
Synthesis and in vitro activity of N′-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists
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
, p. 2093 - 2096 (2008/09/20)
A novel series of cyanoguanidine-piperazine P2X7 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 P2X7 receptors and compound 29 was found to possess potent activity (IC50 = 30-60 nM) at both species.
PIPERAZINES AS P2X7 ANTAGONISTS
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Page/Page column 57, (2008/06/13)
Novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, enantiomers thereof or prodrugs thereof of Formula (I), wherein the substituents are as defined herein, which are useful as therapeutic agen
