| Literature DB >> 19656678 |
Michael D Woodrow1, Stuart P Ballantine, Michael D Barker, Beth J Clarke, John Dawson, Tony W Dean, Christopher J Delves, Brian Evans, Sharon L Gough, Steven B Guntrip, Stuart Holman, Duncan S Holmes, Michael Kranz, Mika K Lindvaal, Fiona S Lucas, Margarete Neu, Lisa E Ranshaw, Yemisi E Solanke, Don O Somers, Peter Ward, Joanne O Wiseman.
Abstract
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-alpha from isolated human peripheral blood mononuclear cells with a pIC(50) of 11.1. GSK256066 also has a suitable profile for inhaled dosing.Entities:
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Year: 2009 PMID： 19656678 DOI： 10.1016/j.bmcl.2009.04.012
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823