1001389-38-3Relevant academic research and scientific papers
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor
Abdi, Muna H.,Beswick, Paul J.,Billinton, Andy,Chambers, Laura J.,Charlton, Andrew,Collins, Sue D.,Collis, Katharine L.,Dean, David K.,Fonfria, Elena,Gleave, Robert J.,Lejeune, Clarisse L.,Livermore, David G.,Medhurst, Stephen J.,Michel, Anton D.,Moses, Andrew P.,Page, Lee,Patel, Sadhana,Roman, Shilina A.,Senger, Stefan,Slingsby, Brian,Steadman, Jon G.A.,Stevens, Alexander J.,Walter, Daryl S.
experimental part, p. 5080 - 5084 (2010/10/04)
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.
Novel Receptor Antagonists and Their Methods of Use
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Page/Page column 34, (2008/06/13)
The present invention relates to novel oxo-prolinamide derivatives of formula (I) which modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
