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. 2010 Sep 1;20(17):5080-4.
doi: 10.1016/j.bmcl.2010.07.033. Epub 2010 Jul 14.

Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor

Muna H Abdi  1 , 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, Andrew P Moses, Lee Page, Sadhana Patel, Shilina A Roman, Stefan Senger, Brian Slingsby, Jon G A Steadman, Alexander J Stevens, Daryl S Walter
Affiliations

Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor

Muna H Abdi et al. Bioorg Med Chem Lett. .

Abstract

A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) 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 P2X(7) antagonist with excellent in vivo activity in animal models of pain, and a profile suitable for progression to clinical studies.

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