Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
DinoprostoneProstaglandin E2 receptor EP1 subtypeKi (nM)9.1N/AN/ADetails
DinoprostoneProstaglandin E2 receptor EP2 subtypeKi (nM)4.9N/AN/ADetails
DinoprostoneProstaglandin E2 receptor EP3 subtypeKi (nM)0.33N/AN/ADetails
DinoprostoneProstaglandin E2 receptor EP4 subtypeEC 50 (nM)3N/AN/ADetails
DinoprostoneProstaglandin E2 receptor EP4 subtypeKi (nM)0.79N/AN/ADetails