Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists
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- 作者：Maria-Jesus Blanco ; blanco_maria@lilly.com" class="auth_mail" title="E-mail the corresponding author ; Tatiana Vetman ; Srinivasan Chandrasekhar ; Matthew J. Fisher ; Anita Harvey ; Daniel Mudra ; Xu-Shan Wang ; Xiao-Peng Yu ; Matthew A. Schiffler ; Alan M. Warshawsky
- 关键词：Arthritis pain ; EP4 receptor antagonist ; Prostaglandin E2 ; Human whole blood assay
- 刊名：Bioorganic & Medicinal Chemistry Letters
- 出版年：2016
- 出版时间：1 January 2016
- 年：2016
- 卷：26
- 期：1
- 页码：105-109
- 全文大小：2017 K
文摘
A novel series of EP4 antagonists, based on a quinoline scaffold, has been discovered. Medicinal chemistry efforts to optimize the potency of the initial hit are described. A highly potent compound in a clinically relevant human whole blood assay was identified. Selectivity and pharmacokinetic profiles of this compound are discussed.