Synthesis and evaluation of novel pyrazolidinone analogs of PGE sub(2) as EP sub(2) and EP sub(4) receptors agonists

Replacement of the hydroxy cyclopentanone ring in PGE sub(2) with chemically more stable heterocyclic rings and substitution of the unsaturated alpha -alkenyl chain with a metabolically more stable phenethyl chain led to the development of potent and selective analogs of PGE sub(2). Compound 10f sho...

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Published inBioorganic & medicinal chemistry Vol. 17; no. 23; pp. 6572 - 6575
Main Authors Zhao, Zhong, Araldi, Gian Luca, Xiao, Yufang, Reddy, Adulla P, Liao, Yihua, Karra, Srinivasa, Brugger, Nadia, Fischer, David, Palmer, Elizabeth
Format Journal Article
LanguageEnglish
Published 01.12.2007
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Summary:Replacement of the hydroxy cyclopentanone ring in PGE sub(2) with chemically more stable heterocyclic rings and substitution of the unsaturated alpha -alkenyl chain with a metabolically more stable phenethyl chain led to the development of potent and selective analogs of PGE sub(2). Compound 10f showed the highest potency and selectivity for EP sub(4) the receptor.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
content type line 23
ObjectType-Feature-2
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmcl.2007.09.074