Discovery of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as glutamine fructose-6-phosphate amidotransferase (GFAT) inhibitors
Through high throughput screening and subsequent hit identification and optimization, we synthesized a series of 1-arylcarbonyl-6,7- dimethoxyisoquinoline derivatives as the first reported potent and reversible GFAT inhibitors. SAR studies of this class o
Potent and selective xanthine-based inhibitors of phosphodiesterase 5
Inhibitors of PDE5 are useful therapeutic agents for treatment of erectile dysfunction. A series of novel xanthine derivatives has been identified as potent inhibitors of PDE5, with good levels of selectivity against other PDE isoforms, including PDE6. St
Arnold, Nichola J.,Arnold, Ruth,Beer, David,Bhalay, Gurdip,Collingwood, Stephen P.,Craig, Sarah,Devereux, Nicholas,Dodds, Mark,Dunstan, Andrew R.,Fairhurst, Robin A.,Farr, David,Fullerton, Joseph D.,Glen, Angela,Gomez, Sylvie,Haberthuer, Sandra,Hatto, Julia D.I.,Howes, Colin,Jones, Darryl,Keller, Thomas H.,Leuenberger, Beate,Moser, Heinz E.,Muller, Irene,Naef, Reto,Nicklin, Paul A.,Sandham, David A.,Turner, Katharine L.,Tweed, Morris F.,Watson, Simon J.,Zurini, Mauro
p. 2376 - 2379
(2007/10/03)
Improved procedures for large preperation of 6- and 7-oxy-substituted isoquinolines and a convenient work-up protocol for titanium supported reactions
Improved procedures for large scale preparation of oxy-substituted isoquinolines are reported. Moreover, a simple and convenient protocol for alkaline work-up of titanium containing reaction mixtures is given, which is expected to be of general interest even for reactions on a technical scale.
Kucznierz, Ralf,Dickhaut, Joachim,Leinert, Herbert,Von Der Saal, Wolfgang
p. 1617 - 1625
(2007/10/03)
Multisubstrate inhibitors of dopamine β-hydroxylase. 2. Structure-activity relationships at the phenethylamine binding site