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

RP Alexander, GJ Warrellow, MAW Eaton… - Bioorganic & medicinal …, 2002 - Elsevier
RP Alexander, GJ Warrellow, MAW Eaton, EC Boyd, JC Head, JR Porter, JA Brown…
Bioorganic & medicinal chemistry letters, 2002Elsevier
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 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.
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 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.
Elsevier