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

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Zhao Z, Araldi GL, Xiao Y, Reddy AP, Liao Y, Karra S, Brugger N, Fischer D, Palmer E

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

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

PubMed ID

17931866 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dinoprostone	Prostaglandin E2 receptor EP2 subtype	Ki (nM)	4.9	N/A	N/A	Details
Dinoprostone	Prostaglandin E2 receptor EP4 subtype	Ki (nM)	0.79	N/A	N/A	Details