Synthesis and evaluation of a γ-lactam as a highly selective EP 2 and EP 4 receptor agonist

…, Z Zhao, A Reddy, S Karra, N Brugger, D Fischer…

Index: Xiao, Yufang; Araldi, Gian Luca; Zhao, Zhong; Reddy, Adulla; Karra, Srinivasa; Brugger, Nadia; Fischer, David; Palmer, Elizabeth; Bao, Bagna; Mckenna, Sean D. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 2 p. 821 - 824

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Citation Number: 14

Abstract

γ-Lactam analogs (2) of EP4 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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