1.
Bioorg Med Chem Lett
; 12(11): 1451-6, 2002 Jun 03.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12031318
RESUMO
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.