Discovery of novel prostaglandin analogs of PGE sub(2) as potent and selective EP sub(2) and EP sub(4) receptor agonists

Analogs of PGE sub(2) with introduction of diene groups at the [Omega]-side chain have been synthesized and evaluated for their binding affinity for EP sub(2) and EP sub(4) receptors. An optimized analog (compound 9b) showed high potency and selectivity for the EP sub(4) receptor over other known re...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007-08, Vol.17 (15), p.4323-4327
Hauptverfasser: Xiao, Yufang, Araldi, Gian Luca, Zhao, Zhong, Brugger, Nadia, Karra, Srinivasa, Fischer, David, Palmer, Elizabeth
Format: Artikel
Sprache:eng
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Zusammenfassung:Analogs of PGE sub(2) with introduction of diene groups at the [Omega]-side chain have been synthesized and evaluated for their binding affinity for EP sub(2) and EP sub(4) receptors. An optimized analog (compound 9b) showed high potency and selectivity for the EP sub(4) receptor over other known receptors.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.05.025