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

  • ACS Med Chem Lett. 2016 Jan 22;7(3):335-9. doi: 10.1021/acsmedchemlett.5b00482.
Huayan Chen  1 ,  Hui Yang  2 ,  Zhilong Wang  2 ,  Xin Xie  2 ,  Fajun Nan  1
Affiliations
  • 1. State Key Laboratory of Drug Research, the National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203, China.
  • 2. CAS Key Laboratory of Receptor Research, the National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203, China.
PMID: 26985325 DOI: 10.1021/acsmedchemlett.5b00482
Abstract

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.

Keywords
CysLT1; CysLT2; Cysteinyl leukotrienes; asthma; selective antagonists.