Article

Synthesis and evaluation of novel pyrazolidinone analogs of PGE(2) as EP2 and EP4 receptors agonists

Department of Medicinal Chemistry, EMD-Serono Research Institute, Inc., Rockland, MA 02370, USA.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.33). 01/2008; 17(23):6572-5. DOI: 10.1016/j.bmcl.2007.09.074
Source: PubMed

ABSTRACT 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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