Discovery of 2-chloro-N-((4, 4-difluoro-1-hydroxycyclohexyl) methyl)-5-(5-fluoropyrimidin-2-yl) benzamide as a potent and CNS penetrable P2X 7 receptor antagonist

X Chen, B Pierce, W Naing, ML Grapperhaus…

Index: Chen, Xiangyang; Pierce, Betsy; Naing, Win; Grapperhaus, Margaret L.; Phillion, Dennis P. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 10 p. 3107 - 3111

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Citation Number: 24

Abstract

Download PDF Opens in a new window. Article suggestions will be shown in a dialog on return to ScienceDirect. ... Please enable JavaScript to use all the features on this page. ... 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 P2X 7 receptor. ... The discovery of a potent P2X 7 receptor antagonist, 7f, with ...