Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
Article Details
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Xiao Y, Araldi GL, Zhao Z, Reddy A, Karra S, Brugger N, Fischer D, Palmer E, Bao B, McKenna SD
Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
Bioorg Med Chem Lett. 2008 Jan 15;18(2):821-4. Epub 2007 Nov 13.
- PubMed ID
- 18039575 [ View in PubMed]
- Abstract
Gamma-lactam analogs (2) of EP(4) receptor agonists were identified by substitution of the pyrazolidinone ring (1) with a pyrrolidinone ring. Several compounds (such as 2a, 2h) with high potency, selectivity and acceptable PK profiles were discovered. These were assessed in animal models of ovulation induction and bronchoconstriction.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Dinoprostone Prostaglandin E2 receptor EP1 subtype Ki (nM) 9.1 N/A N/A Details Dinoprostone Prostaglandin E2 receptor EP2 subtype Ki (nM) 4.9 N/A N/A Details Dinoprostone Prostaglandin E2 receptor EP3 subtype Ki (nM) 0.33 N/A N/A Details Dinoprostone Prostaglandin E2 receptor EP4 subtype EC 50 (nM) 3 N/A N/A Details Dinoprostone Prostaglandin E2 receptor EP4 subtype Ki (nM) 0.79 N/A N/A Details