229184-01-4Relevant articles and documents
Tricyclic pyridones as functionally selective human GABA Aα2/3 receptor-ion channel ligands
Crawforth, James,Atack, John R.,Cook, Susan M.,Gibson, Karl R.,Nadin, Alan,Owens, Andrew P.,Pike, Andrew,Rowley, Michael,Smith, Alison J.,Sohal, Bindi,Sternfeld, Francine,Wafford, Keith,Street, Leslie J.
, p. 1679 - 1682 (2007/10/03)
A series of tricyclic pyridones has been evaluated as benzodiazepine site ligands with functional selectivity for the α3 over the α1 containing subtype of the human GABAA receptor ion channel. This investigation led to the
Synthesis and conformational dynamics of tricyclic pyridones containing a fused seven-membered ring
Gibson, Karl R.,Hitzel, Laure,Mortishire-Smith, Russell J.,Gerhard, Ute,Jelley, Richard A.,Reeve, Austin J.,Rowley, Michael,Nadin, Alan,Owens, Andrew P.
, p. 9354 - 9360 (2007/10/03)
A new synthetic approach to tricyclic pyridones bearing a fused seven-membered ring is described. These compounds exhibit atropisomerism and exist in enantiomeric forms. Chiral HPLC separation of the enantiomers has allowed the rates of racemization to be measured and hence the free energy barrier for flipping the seven-membered ring to be deduced. Introduction of a further element of planar chirality leads to diastereomeric atropisomerism. The rate of interconversion of the diastereomers has been quantified by 2D EXSY NMR spectroscopy allowing a full description of the conformational dynamics of the system.
