Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.
ID: CHEMBL1140555
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.
Authors: Zhao Z, Araldi GL, Xiao Y, Reddy AP, Liao Y, Karra S, Brugger N, Fischer D, Palmer E.
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.
CiteXplore: 17931866
Patent ID: ---
Protein Target Summary
Total
11
Eukaryotes
N/A
Assay Summary
Total
17
A - ADME
B - Binding
F - Functional
P - Physicochemical
Bioactivity Summary
Total
68
Ki
EC50
Selectivity ratio
Solubility
Stability
Activity
CL
F
Fu
PPB
Papp
T1/2
Vd
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