1.
Bioorg Med Chem Lett
; 20(17): 5080-4, 2010 Sep 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-20673717
RESUMEN
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.