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

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

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 sub(7) receptor.

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-05, Vol.20 (10), p.3107-3111
Hauptverfasser: Chen, Xiangyang, Pierce, Betsy, Naing, Win, Grapperhaus, Margaret L, Phillion, Dennis P
Format: Artikel
Sprache:eng
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Zusammenfassung: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 sub(7) receptor.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.03.094