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

Authors :
Xiao, Yufang
Araldi, Gian Luca
Zhao, Zhong
Reddy, Adulla
Karra, Srinivasa
Brugger, Nadia
Fischer, David
Palmer, Elizabeth
Bao, Bagna
Mckenna, Sean D.
Source :
Bioorganic & Medicinal Chemistry Letters. Jan2008, Vol. 18 Issue 2, p821-824. 4p.
Publication Year :
2008

Abstract

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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
18
Issue :
2
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
28611880
Full Text :
https://doi.org/10.1016/j.bmcl.2007.11.020