3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP 3 receptor antagonists

Yue H. Li; Pei San Tseng; Karen A. Evans; Jon Paul Jaworski; Dwight M. Morrow; Harvey E. Fries; Charlene W. Wu; Richard M. Edwards; Jian Jin

doi:10.1016/j.bmcl.2010.08.137

3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP ₃ receptor antagonists

Yue H. Li
, Pei San Tseng
, Karen A. Evans
, Jon Paul Jaworski
, Dwight M. Morrow
, Harvey E. Fries
, Charlene W. Wu
, Richard M. Edwards
, Jian Jin

Research output: Contribution to journal › Article › peer-review

7 Scopus citations

Abstract

A series of 3-urea-1-(phenylmethyl)-pyridones was discovered as novel EP₃ antagonists via high-throughput screening and subsequent optimization. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in potent and selective EP₃ receptor antagonists such as 11g are described.

Original language	English
Pages (from-to)	6744-6747
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	22
DOIs	https://doi.org/10.1016/j.bmcl.2010.08.137
State	Published - 15 Nov 2010
Externally published	Yes

Keywords

3-Urea-1-(phenylmethyl)-pyridones
Antagonists
EP
Prostaglandins

Access to Document

10.1016/j.bmcl.2010.08.137

Cite this

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title = "3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP 3 receptor antagonists",

abstract = "A series of 3-urea-1-(phenylmethyl)-pyridones was discovered as novel EP3 antagonists via high-throughput screening and subsequent optimization. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in potent and selective EP3 receptor antagonists such as 11g are described.",

keywords = "3-Urea-1-(phenylmethyl)-pyridones, Antagonists, EP, Prostaglandins",

author = "Li, \{Yue H.\} and Tseng, \{Pei San\} and Evans, \{Karen A.\} and Jaworski, \{Jon Paul\} and Morrow, \{Dwight M.\} and Fries, \{Harvey E.\} and Wu, \{Charlene W.\} and Edwards, \{Richard M.\} and Jian Jin",

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AU - Li, Yue H.

AU - Tseng, Pei San

AU - Evans, Karen A.

AU - Jaworski, Jon Paul

AU - Morrow, Dwight M.

AU - Fries, Harvey E.

AU - Wu, Charlene W.

AU - Edwards, Richard M.

AU - Jin, Jian

PY - 2010/11/15

Y1 - 2010/11/15

N2 - A series of 3-urea-1-(phenylmethyl)-pyridones was discovered as novel EP3 antagonists via high-throughput screening and subsequent optimization. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in potent and selective EP3 receptor antagonists such as 11g are described.

AB - A series of 3-urea-1-(phenylmethyl)-pyridones was discovered as novel EP3 antagonists via high-throughput screening and subsequent optimization. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in potent and selective EP3 receptor antagonists such as 11g are described.

KW - 3-Urea-1-(phenylmethyl)-pyridones

KW - Antagonists

KW - EP

KW - Prostaglandins

UR - https://www.scopus.com/pages/publications/77958027410

U2 - 10.1016/j.bmcl.2010.08.137

DO - 10.1016/j.bmcl.2010.08.137

M3 - Article

C2 - 20926294

AN - SCOPUS:77958027410

SN - 0960-894X

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JO - Bioorganic and Medicinal Chemistry Letters

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