792912-14-2Relevant articles and documents
Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X7 receptor
Subramanyam, Chakrapani,Duplantier, Allen J.,Dombroski, Mark A.,Chang, Shang-Poa,Gabel, Christopher A.,Whitney-Pickett, Carrie,Perregaux, David G.,Labasi, Jeff M.,Yoon, Kwansik,Shepard, Richard M.,Fisher, Michael
, p. 5475 - 5479 (2011/10/12)
The discovery, of a series of 2-Cl-5-heteroaryl-benzamide antagonists of the P2X7 receptor via parallel medicinal chemistry is described. Initial analogs suffered from poor metabolic stability and low Vdss. Multi parametric optimizat
Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist
Chen, Xiangyang,Pierce, Betsy,Naing, Win,Grapperhaus, Margaret L.,Phillion, Dennis P.
scheme or table, p. 3107 - 3111 (2010/09/03)
Focused SAR studies were carried out around 5-heteroaryl and 1-amide portions of the 2-chlorobenzamide scaffold, resulting in the discovery of a potent, metabolically stable and centrally penetrable antagonist against P2X7 receptor.