1001389-29-2Relevant 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.
