N-Substituted phenoxazine and acridone derivatives: structure–activity relationships of potent P2X4 receptor antagonists

V Hernandez-Olmos, A Abdelrahman…

Index: Hernandez-Olmos, Victor; Abdelrahman, Aliaa; El-Tayeb, Ali; Freudendahl, Diana; Weinhausen, Stephanie; Mueller, Christa E. Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9576 - 9588

Full Text: HTML

Citation Number: 30

Abstract

P2X4 receptor antagonists have potential as drugs for the treatment of neuropathic pain and neurodegenerative diseases. In the present study the discovery of phenoxazine derivatives as potent P2X4 antagonists is described. N-Substituted phenoxazine and related acridone and benzoxazine derivatives were synthesized and optimized with regard to their potency to inhibit ATP-induced calcium influx in 1321N1 astrocytoma cells stably transfected with the ...