Literature DB >> 14592505

Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists.

Andrew Baxter1, Janice Bent, Keith Bowers, Martin Braddock, Steve Brough, Malbinder Fagura, Mandy Lawson, Tom McInally, Mike Mortimore, Mark Robertson, Richard Weaver, Peter Webborn.   

Abstract

A Hit-to-Lead optimisation programme was carried out on the adamantane high throughput screening hit 1 resulting in the discovery of a number of potent P2X(7) antagonists.

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Year:  2003        PMID: 14592505     DOI: 10.1016/j.bmcl.2003.08.034

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


  23 in total

Review 1.  The first CNS-active carborane: A novel P2X7 receptor antagonist with antidepressant activity.

Authors:  Shane M Wilkinson; Hendra Gunosewoyo; Melissa L Barron; Aurelie Boucher; Michelle McDonnell; Peter Turner; Daniel E Morrison; Maxwell R Bennett; Iain S McGregor; Louis M Rendina; Michael Kassiou
Journal:  ACS Chem Neurosci       Date:  2014-04-03       Impact factor: 4.418

2.  Identification of Thr283 as a key determinant of P2X7 receptor function.

Authors:  M T Young; P Pelegrin; A Surprenant
Journal:  Br J Pharmacol       Date:  2006-08-29       Impact factor: 8.739

Review 3.  Pharmacology of P2X channels.

Authors:  Joel R Gever; Debra A Cockayne; Michael P Dillon; Geoffrey Burnstock; Anthony P D W Ford
Journal:  Pflugers Arch       Date:  2006-04-29       Impact factor: 3.657

4.  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

Review 5.  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

Review 6.  Agonists and antagonists for P2 receptors.

Authors:  Kenneth A Jacobson; Stefano Costanzi; Bhalchandra V Joshi; Pedro Besada; Dae Hong Shin; Hyojin Ko; Andrei A Ivanov; Liaman Mamedova
Journal:  Novartis Found Symp       Date:  2006

Review 7.  Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states.

Authors:  D L Donnelly-Roberts; M F Jarvis
Journal:  Br J Pharmacol       Date:  2007-04-30       Impact factor: 8.739

8.  Reanalysis of P2X7 receptor expression in rodent brain.

Authors:  Joan A Sim; Mark T Young; Hye-Youn Sung; R Alan North; Annmarie Surprenant
Journal:  J Neurosci       Date:  2004-07-14       Impact factor: 6.167

9.  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

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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