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Bioorg Med Chem Lett. 2008 Jan 15;18(2):821-4. Epub 2007 Nov 13.

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

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  • 1Department of Medicinal Chemistry, EMD-Serono Research Institute, Inc., Rockland, MA 02370, USA.


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.

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