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Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jan 15; Vol. 18 (2), pp. 821-4. Date of Electronic Publication: 2007 Nov 13. - Publication Year :
- 2008
-
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.
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18039575
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.11.020