Literature DB >> 20137946

Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists.

Paul Eastwood1, Jacob Gonzalez, Sergio Paredes, Arsenio Nueda, Teresa Domenech, Joan Alberti, Bernat Vidal.   

Abstract

The synthesis and SAR of a series of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent A(2B) adenosine receptor antagonists is described. Several compounds showed good selectivity versus other adenosine receptors. The potent and selective analogue 9 was shown to have good oral bioavailability in the rat. Copyright 2010 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 20137946     DOI： 10.1016/j.bmcl.2010.01.045

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

Review 1.  Recent developments in adenosine receptor ligands and their potential as novel drugs.

Authors:  Christa E Müller; Kenneth A Jacobson
Journal:  Biochim Biophys Acta       Date:  2010-12-23

Review 2.  International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.

Authors:  Bertil B Fredholm; Adriaan P IJzerman; Kenneth A Jacobson; Joel Linden; Christa E Müller
Journal:  Pharmacol Rev       Date:  2011-02-08       Impact factor: 25.468

3.  Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist.

Authors:  Paul Eastwood; Cristina Esteve; Jacob González; Silvia Fonquerna; Josep Aiguadé; Inés Carranco; Teresa Doménech; Mònica Aparici; Montserrat Miralpeix; Joan Albertí; Mónica Córdoba; Raquel Fernández; Mercè Pont; Núria Godessart; Neus Prats; María Isabel Loza; María Isabel Cadavid; Arsenio Nueda; Bernat Vidal
Journal:  ACS Med Chem Lett       Date:  2010-12-20       Impact factor: 4.345

4.  Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists.

Authors:  Abel Crespo; Abdelaziz El Maatougui; Pierfrancesco Biagini; Jhonny Azuaje; Alberto Coelho; José Brea; María Isabel Loza; María Isabel Cadavid; Xerardo García-Mera; Hugo Gutiérrez-de-Terán; Eddy Sotelo
Journal:  ACS Med Chem Lett       Date:  2013-10-03       Impact factor: 4.345

5.  Chemoselective Synthesis of Polysubstituted Pyridines from Heteroaryl Fluorosulfates.

Authors:  Enxuan Zhang; Jiaze Tang; Suhua Li; Peng Wu; John E Moses; K Barry Sharpless
Journal:  Chemistry       Date:  2016-03-15       Impact factor: 5.236

6.  Site-selective Suzuki-Miyaura coupling of heteroaryl halides - understanding the trends for pharmaceutically important classes.

Authors:  Joshua Almond-Thynne; David C Blakemore; David C Pryde; Alan C Spivey
Journal:  Chem Sci       Date:  2016-08-09       Impact factor: 9.825

7.  Development of a Radiofluorinated Adenosine A2B Receptor Antagonist as Potential Ligand for PET Imaging.

Authors:  Marcel Lindemann; Rareş-Petru Moldovan; Sonja Hinz; Winnie Deuther-Conrad; Daniel Gündel; Sladjana Dukic-Stefanovic; Magali Toussaint; Rodrigo Teodoro; Cathleen Juhl; Jörg Steinbach; Peter Brust; Christa E Müller; Barbara Wenzel
Journal:  Int J Mol Sci       Date:  2020-04-30       Impact factor: 5.923
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.