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

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 (IC50 4 nM). CDP840 is non-emetic in the ferret at 30 mg kg−1 (po), active in models of inflammation and reverses ozone-induced bronchial hyperreactivity in the guinea pig. [Copyright &y& Elsevier]