| Abstract
| - Two novel classes of diphenyloxazole and Nδ-Z-ornithine derivatives as highly potent and selective EP4antagonists have been discovered. The optimized diphenyloxzole 8 and Nδ-Z-ornithine 11 effectively competed with [3H]PGE2 binding to human recombinant EP4, with Ki values of0.30 nM and 0.91 nM, respectively, and were selective for allmembers of the human prostanoid receptor family. 8 wasshown to exhibit good pharmacokinetic properties in rats anddogs and potent inhibitory activity toward in vitro PGE2-promoted IgE synthesis.
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