871819-53-3Relevant articles and documents
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin- 7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain
Giblin, Gerard M. P.,Billinton, Andrew,Briggs, Michael,Brown, Andrew J.,Chessell, Iain P.,Clayton, Nick M.,Eatherton, Andrew J.,Goldsmith, Paul,Haslam, Carl,Johnson, Matthew R.,Mitchell, William L.,Naylor, Alan,Perboni, Alcide,Slingsby, Brian P.,Wilson, Alex W.
, p. 5785 - 5788 (2009)
We report the synthesis and SAR of a series of novel azaindole CB 2 agonists. 6-Azaindole 18 showed activity in an acute pain model but was inactive in a chronic model. 18 is a Pgp substrate with low brain penetration. The template was redesign