Journal article Open Access

Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X7 receptor antagonists.

Wong, Erick CN; Reekie, Tristan A; Werry, Eryn L; O'Brien-Brown, James; Bowyer, Sarah L; Kassiou, Michael

Abstract

We report on P2X7 receptor antagonists based on a lead adamantly-cyanoguanidine-aryl moiety. We have investigated the importance of the central cyanoguanidine moiety by replacing it with urea, thiourea or guanidine moieties. We have also investigated the linker length between the central moiety and the aryl portion. All compounds were assessed for their inhibitory potency in a pore-formation dye uptake assay at the P2X7 receptor. None of the compounds resulted in an improved potency illustrating the importance of the cyanoguanidine moiety in this chemotype.

Files (342.1 kB)
Name Size
Wong_BMCL_2017-P19-AAM.pdf
md5:178a4f5e5e57f4843ad0cbf19ced3c1a
342.1 kB Download
11
7
views
downloads
Views 11
Downloads 7
Data volume 2.4 MB
Unique views 11
Unique downloads 7

Share

Cite as