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. 2002 Jun 3;12(11):1451-6.
doi: 10.1016/s0960-894x(02)00202-0.

CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors

R P Alexander  1 , G J Warrellow, M A W Eaton, E C Boyd, J C Head, J R Porter, J A Brown, J T Reuberson, B Hutchinson, P Turner, B Boyce, D Barnes, B Mason, A Cannell, R J Taylor, A Zomaya, A Millican, J Leonard, R Morphy, M Wales, M Perry, R A Allen, N Gozzard, B Hughes, G Higgs
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CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors

R P Alexander et al. Bioorg Med Chem Lett. .

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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