25391-59-7Relevant articles and documents
5-Azidoepibatidine: An Exceptionally Potent Photoaffinity Ligand for Neuronal α4β2 and α7 Nicotinic Acetylcholine Receptors
Zhang, Nanjing,Tomizawa, Motohiro,Casida, John E.
, p. 525 - 528 (2003)
Racemic 5-azidoepibatidine [(+/-)-1] was synthesized via 5-aminoepibatidine as a candidate photoaffinity ligand with exceptionally high affinity at the mammalian neuronal nicotinic receptors (Ki values of 0.027 nM for α4β2 and 9.7 nM for α7) and excellent photoreactivity.
ANTI-FIBROTIC PYRIDINONES
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Paragraph 0656-0657, (2014/04/17)
Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
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.
supporting information; experimental part, p. 5785 - 5788 (2010/02/28)
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