Literature DB >> 26985325

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

Huayan Chen1, Hui Yang2, Zhilong Wang2, Xin Xie2, Fajun Nan1.   

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.

Entities:  

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

Year:  2016        PMID： 26985325      PMCID： PMC4789669          DOI： 10.1021/acsmedchemlett.5b00482

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  19 in total

Review 1.  Leukotrienes.

Authors:  Marc Peters-Golden; William R Henderson
Journal:  N Engl J Med       Date:  2007-11-01       Impact factor: 91.245

2.  Characterization of the human cysteinyl leukotriene CysLT1 receptor.

Authors:  K R Lynch; G P O'Neill; Q Liu; D S Im; N Sawyer; K M Metters; N Coulombe; M Abramovitz; D J Figueroa; Z Zeng; B M Connolly; C Bai; C P Austin; A Chateauneuf; R Stocco; G M Greig; S Kargman; S B Hooks; E Hosfield; D L Williams; A W Ford-Hutchinson; C T Caskey; J F Evans
Journal:  Nature       Date:  1999-06-24       Impact factor: 49.962

3.  Expression of CysLT2 receptors in asthma lung, and their possible role in bronchoconstriction.

Authors:  Tomohiko Sekioka; Michiaki Kadode; Masanori Fujii; Kazuhito Kawabata; Takashi Abe; Michiaki Horiba; Shigekatsu Kohno; Takeshi Nabe
Journal:  Allergol Int       Date:  2015-06-03       Impact factor: 5.836

4.  Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17.

Authors:  Meryem Köse; Kirsten Ritter; Katharina Thiemke; Michel Gillard; Evi Kostenis; Christa E Müller
Journal:  ACS Med Chem Lett       Date:  2014-01-16       Impact factor: 4.345

5.  Cysteinyl leukotrienes induce human eosinophil locomotion and adhesion molecule expression via a CysLT1 receptor-mediated mechanism.

Authors:  L Fregonese; M Silvestri; F Sabatini; G A Rossi
Journal:  Clin Exp Allergy       Date:  2002-05       Impact factor: 5.018

6.  A selective cysteinyl leukotriene receptor 2 antagonist blocks myocardial ischemia/reperfusion injury and vascular permeability in mice.

Authors:  Nathan C Ni; Dong Yan; Laurel L Ballantyne; Alma Barajas-Espinosa; Tim St Amand; Derek A Pratt; Colin D Funk
Journal:  J Pharmacol Exp Ther       Date:  2011-09-08       Impact factor: 4.030

7.  Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.

Authors:  R Di Fabio; A M Capelli; N Conti; A Cugola; D Donati; A Feriani; P Gastaldi; G Gaviraghi; C T Hewkin; F Micheli; A Missio; M Mugnaini; A Pecunioso; A M Quaglia; E Ratti; L Rossi; G Tedesco; D G Trist; A Reggiani
Journal:  J Med Chem       Date:  1997-03-14       Impact factor: 7.446

8.  Leukotriene D(4) induces gene expression in human monocytes through cysteinyl leukotriene type I receptor.

Authors:  Grzegorz Woszczek; Li-Yuan Chen; Sahrudaya Nagineni; Steven Kern; Jennifer Barb; Peter J Munson; Carolea Logun; Robert L Danner; James H Shelhamer
Journal:  J Allergy Clin Immunol       Date:  2007-10-29       Impact factor: 10.793

Review 9.  Functional characteristics of cysteinyl-leukotriene receptor subtypes.

Authors:  Magnus Bäck
Journal:  Life Sci       Date:  2002-06-28       Impact factor: 5.037

10.  Structural and functional rejuvenation of the aged brain by an approved anti-asthmatic drug.

Authors:  Julia Marschallinger; Iris Schäffner; Barbara Klein; Renate Gelfert; Francisco J Rivera; Sebastian Illes; Lukas Grassner; Maximilian Janssen; Peter Rotheneichner; Claudia Schmuckermair; Roland Coras; Marta Boccazzi; Mansoor Chishty; Florian B Lagler; Marija Renic; Hans-Christian Bauer; Nicolas Singewald; Ingmar Blümcke; Ulrich Bogdahn; Sebastien Couillard-Despres; D Chichung Lie; Maria P Abbracchio; Ludwig Aigner
Journal:  Nat Commun       Date:  2015-10-27       Impact factor: 14.919
View more
  3 in total

1.  Boosting Intracellular Delivery of Lipid Nanoparticle-Encapsulated mRNA.

Authors:  Siddharth Patel; N Ashwanikumar; Emily Robinson; Allison DuRoss; Conroy Sun; Kerry E Murphy-Benenato; Cosmin Mihai; Örn Almarsson; Gaurav Sahay
Journal:  Nano Lett       Date:  2017-08-24       Impact factor: 11.189

2.  Novel 15-Lipoxygenase-1 Inhibitor Protects Macrophages from Lipopolysaccharide-Induced Cytotoxicity.

Authors:  Hao Guo; Iris C Verhoek; Gerian G H Prins; Ramon van der Vlag; Petra E van der Wouden; Ronald van Merkerk; Wim J Quax; Peter Olinga; Anna K H Hirsch; Frank J Dekker
Journal:  J Med Chem       Date:  2019-04-19       Impact factor: 7.446

3.  Design, synthesis, in vitro antiproliferative activity and apoptosis-inducing studies of 1-(3',4',5'-trimethoxyphenyl)-3-(2'-alkoxycarbonylindolyl)-2-propen-1-one derivatives obtained by a molecular hybridisation approach.

Authors:  Delia Preti; Romeo Romagnoli; Riccardo Rondanin; Barbara Cacciari; Ernest Hamel; Jan Balzarini; Sandra Liekens; Dominique Schols; Francisco Estévez-Sarmiento; José Quintana; Francisco Estévez
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.