807325-73-1Relevant academic research and scientific papers
Repurposing human PDE4 inhibitors for neglected tropical diseases. evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of pdeb1 of trypanosoma brucei
Ochiana, Stefan O.,Bland, Nicholas D.,Settimo, Luca,Campbell, Robert K.,Pollastri, Michael P.
, p. 549 - 564 (2015/04/22)
Cyclic nucleotide phosphodiesterases (PDEs) have been identified as important enzyme targets for drug development in both humans and Trypanosoma brucei, the causative agent of human African trypanosomiasis. With this in mind, we recently reported the prof
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration
Woodrow, Michael D.,Ballantine, Stuart P.,Barker, Michael D.,Clarke, Beth J.,Dawson, John,Dean, Tony W.,Delves, Christopher J.,Evans, Brian,Gough, Sharon L.,Guntrip, Steven B.,Holman, Stuart,Holmes, Duncan S.,Kranz, Michael,Lindvaal, Mika K.,Lucas, Fiona S.,Neu, Margarete,Ranshaw, Lisa E.,Solanke, Yemisi E.,Somers, Don O.,Ward, Peter,Wiseman, Joanne O.
scheme or table, p. 5261 - 5265 (2010/03/31)
Crystallography driven optimisation of a lead derived from similarity searching of the GSK compound collection resulted in the discovery of quinoline-3-carboxamides as highly potent and selective inhibitors of phosphodiesterase 4B. This series has been optimized to GSK256066, a potent PDE4B inhibitor which also inhibits LPS induced production of TNF-α from isolated human peripheral blood mononuclear cells with a pIC50 of 11.1. GSK256066 also has a suitable profile for inhaled dosing.
