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

✍ Scribed by 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; Andrew P. Moses; Lee Page; Sadhana Patel; Shilina A. Roman; Stefan Senger; Brian Slingsby; Jon G.A. Steadman; Alexander J. Stevens; Daryl S. Walter

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 720 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.033

No coin nor oath required. For personal study only.

✦ Synopsis

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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