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Bioorg Med Chem Lett. 2002 Jun 3;12(11):1451-6.

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

Author information

1
Department of Medicinal Chemistry, Celltech R&D Ltd., 208 Bath Road, Slough, Berkshire SL1 3WE, UK. rikki.alexander@celltechgroup.com

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.

PMID:
12031318
DOI:
10.1016/s0960-894x(02)00202-0
[Indexed for MEDLINE]

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