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Bioorganic & medicinal chemistry letters

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


PMID 18039575

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.