Literature DB >> 17963373

Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.

Mark Furber1, Lilian Alcaraz, Janice E Bent, Armin Beyerbach, Keith Bowers, Martin Braddock, Moya V Caffrey, David Cladingboel, John Collington, David K Donald, Malbinder Fagura, Frank Ince, Elizabeth C Kinchin, Celine Laurent, Mandy Lawson, Timothy J Luker, Michael M P Mortimore, Austen D Pimm, Robert J Riley, Nicola Roberts, Mark Robertson, Jill Theaker, Philip V Thorne, Richard Weaver, Peter Webborn, Paul Willis.   

Abstract

A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.

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Year:  2007        PMID: 17963373     DOI: 10.1021/jm700949w

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  14 in total

1.  Molecular characterization, gas chromatography mass spectrometry analysis, phytochemical screening and insecticidal activities of ethanol extract of Lentinus squarrosulus against Aedes aegypti (Linnaeus).

Authors:  Morenike Olutumbi Adeoye-Isijola; Segun Gbolagade Jonathan; Roger Murugas Coopoosamy; Olufunmiso Olusola Olajuyigbe
Journal:  Mol Biol Rep       Date:  2021-01-17       Impact factor: 2.316

2.  Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567.

Authors:  Anindya Bhattacharya; Qi Wang; Hong Ao; James R Shoblock; Brian Lord; Leah Aluisio; Ian Fraser; Diane Nepomuceno; Robert A Neff; Natalie Welty; Timothy W Lovenberg; Pascal Bonaventure; Alan D Wickenden; Michael A Letavic
Journal:  Br J Pharmacol       Date:  2013-10       Impact factor: 8.739

3.  P2X(7) Receptors in Neurological and Cardiovascular Disorders.

Authors:  Stephen D Skaper; Patrizia Debetto; Pietro Giusti
Journal:  Cardiovasc Psychiatry Neurol       Date:  2009-06-24

Review 4.  The lipophilic bullet hits the targets: medicinal chemistry of adamantane derivatives.

Authors:  Lukas Wanka; Khalid Iqbal; Peter R Schreiner
Journal:  Chem Rev       Date:  2013-02-25       Impact factor: 60.622

5.  Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.

Authors:  Michael A Letavic; Brian Lord; Francois Bischoff; Natalie A Hawryluk; Serge Pieters; Jason C Rech; Zachary Sales; Adriana I Velter; Hong Ao; Pascal Bonaventure; Victor Contreras; Xiaohui Jiang; Kirsten L Morton; Brian Scott; Qi Wang; Alan D Wickenden; Nicholas I Carruthers; Anindya Bhattacharya
Journal:  ACS Med Chem Lett       Date:  2013-03-12       Impact factor: 4.345

6.  Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists.

Authors:  Brad M Savall; Duncan Wu; Meri De Angelis; Nicholas I Carruthers; Hong Ao; Qi Wang; Brian Lord; Anindya Bhattacharya; Michael A Letavic
Journal:  ACS Med Chem Lett       Date:  2015-04-24       Impact factor: 4.345

7.  Identification and characterization of a novel variant of the human P2X(7) receptor resulting in gain of function.

Authors:  Chengqun Sun; Jessica Chu; Sarita Singh; Russell D Salter
Journal:  Purinergic Signal       Date:  2009-10-17       Impact factor: 3.765

8.  Synthesis of spiroannulated and 3-arylated 1,2,4-trioxanes from mesitylol and methyl 4-hydroxytiglate by photooxygenation and peroxyacetalization.

Authors:  Axel G Griesbeck; Lars-Oliver Höinck; Jörg M Neudörfl
Journal:  Beilstein J Org Chem       Date:  2010-06-07       Impact factor: 2.883

9.  Mechanism of action of species-selective P2X(7) receptor antagonists.

Authors:  Anton D Michel; Sin-Wei Ng; Shilina Roman; William C Clay; David K Dean; Daryl S Walter
Journal:  Br J Pharmacol       Date:  2009-03-20       Impact factor: 8.739

10.  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

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