Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists

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• 作者：Huayan Chen ; Hui Yang ; Zhilong Wang ; Xin Xie ; Fajun Nan
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：March 10, 2016
• 年：2016
• 卷：7
• 期：3
• 页码：335-339
• 全文大小：375K
• ISSN：1948-5875

文摘

The indole derivative, 3-((E)-3-((3-((E)-2-(7-chloroquinolin-2yl)vinyl)phenyl)amino)-3-oxoprop-1-en-1-yl)-7-methoxy-1H-indole-2-carboxylic acid (17k), was identified as a novel and highly potent and selective CysLT₁ antagonist with IC₅₀ values of 0.0059 ± 0.0011 and 15 ± 4 μM for CysLT₁ and CysLT₂, respectively.