| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374625 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X7 receptor antagonist. Structure–activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and compound 31 was identified as a potent P2X7 antagonist with excellent in vivo activity in animal models of pain, and a profile suitable for progression to clinical studies.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Muna H. Abdi, Paul J. Beswick, Andy Billinton, Laura J. Chambers, Andrew Charlton, Sue D. Collins, Katharine L. Collis, David K. Dean, Elena Fonfria, Robert J. Gleave, Clarisse L. Lejeune, David G. Livermore, Stephen J. Medhurst, Anton D. Michel,