Literature DB >> 18272365

Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists.

Michael J Morytko1, Patrick Betschmann, Kevin Woller, Anna Ericsson, Haipeng Chen, Diana L Donnelly-Roberts, Marian T Namovic, Michael F Jarvis, William A Carroll, Paul Rafferty.   

Abstract

A novel series of cyanoguanidine-piperazine P2X(7) 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 P2X(7) receptors and compound 29 was found to possess potent activity (IC(50)=30-60 nM) at both species.

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Year:  2008        PMID： 18272365     DOI： 10.1016/j.bmcl.2008.01.094

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Activation and regulation of purinergic P2X receptor channels.

Authors:  Claudio Coddou; Zonghe Yan; Tomas Obsil; J Pablo Huidobro-Toro; Stanko S Stojilkovic
Journal:  Pharmacol Rev       Date:  2011-07-07       Impact factor: 25.468

2.  Design, synthesis and evaluation in an LPS rodent model of neuroinflammation of a novel 18F-labelled PET tracer targeting P2X7.

Authors:  Enrico Raffaele Fantoni; Diego Dal Ben; Simonetta Falzoni; Francesco Di Virgilio; Simon Lovestone; Antony Gee
Journal:  EJNMMI Res       Date:  2017-04-04       Impact factor: 3.138

3.  Selective P2X(7) receptor antagonists for chronic inflammation and pain.

Authors:  William A Carroll; Diana Donnelly-Roberts; Michael F Jarvis
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765
  3 in total

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