Quinolines as a novel structural class of potent and selective PDE4 inhibitors: Optimisation for oral administration
2009; Elsevier BV; Volume: 19; Issue: 5 Linguagem: Inglês
10.1016/j.bmcl.2009.01.045
ISSN1464-3405
AutoresMichael D. Woodrow, Stuart P. Ballantine, Michael D. Barker, Beth J. Clarke, John Dawson, Tony W. Dean, C. 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 Solanke, Don O. Somers, Peter Ward, Joanne Wiseman,
Tópico(s)Enzyme function and inhibition
ResumoCrystallography-driven optimisation of a lead derived from similarity searching of the GSK compound collection resulted in the discovery of a series of quinoline derivatives that were highly potent and selective inhibitors of PDE4 with a good pharmacokinetic profile in the rat. Quinolines 43 and 48 have potential as oral medicines for the treatment of COPD
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