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

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 ovulatio...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008-01, Vol.18 (2), p.821-824
Hauptverfasser:	YUFANG XIAO, LUCA ARALDI, Gian, ZHONG ZHAO, REDDY, Adulla, KARRA, Srinivasa, BRUGGER, Nadia, FISCHER, David, PALMER, Elizabeth, BAO, Bagna, MCKENNA, Sean D
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Female Genital system. Reproduction Guinea Pigs Humans Lactams - chemical synthesis Lactams - pharmacokinetics Lactams - pharmacology Male Medical sciences Mice Ovulation Induction Pharmacology. Drug treatments Receptors, Prostaglandin E - agonists Receptors, Prostaglandin E, EP2 Subtype Receptors, Prostaglandin E, EP4 Subtype Respiratory system Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.11.020