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Bioorg Med Chem Lett. 2007 Dec 1;17(23):6572-5. Epub 2007 Sep 26.

Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.

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  • 1Department of Medicinal Chemistry, EMD-Serono Research Institute, Inc., Rockland, MA 02370, USA.


Replacement of the hydroxy cyclopentanone ring in PGE(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(2). Compound 10f showed the highest potency and selectivity for EP(4) the receptor.

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