CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors |
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| Authors: | Alexander R P Warrellow G J Eaton M A W Boyd E C Head J C Porter J R Brown J A Reuberson J T Hutchinson B Turner P Boyce B Barnes D Mason B Cannell A Taylor R J Zomaya A Millican A Leonard J Morphy R Wales M Perry M Allen R A Gozzard N Hughes B Higgs G |
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| Institution: | Department of Medicinal Chemistry, Celltech R&D Ltd., 208 Bath Road, Slough, Berkshire SL1 3WE, UK. rikki.alexander@celltechgroup.com |
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| Abstract: | The discovery, synthesis and biological activity of a series of triarylethane phosphodiesterase 4 inhibitors is described. Structure-activity relationship studies are presented for CDP840 (29), a potent, chiral, selective inhibitor of PDE 4 (IC(50) 4nM). CDP840 is non-emetic in the ferret at 30mgkg(-1) (po), active in models of inflammation and reverses ozone-induced bronchial hyperreactivity in the guinea pig. |
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