Literature DB >> 17469811

Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.

Bernat Vidal1, Arsenio Nueda, Cristina Esteve, Teresa Domenech, Sonia Benito, Raquel F Reinoso, Mercè Pont, Marta Calbet, Rosa López, María Isabel Cadavid, María Isabel Loza, Alvaro Cárdenas, Núria Godessart, Jorge Beleta, Graham Warrellow, Hamish Ryder.   

Abstract

A novel series of N-heteroaryl 4'-(2-furyl)-4,5'-bipyrimidin-2'-amines has been identified as potent and selective A(2B) adenosine receptor antagonists. In particular, compound 5 showed high affinity for the A(2B) receptor (Ki = 17 nM), good selectivity (IC(50): A(1) > 1000 nM, A(2A) > 2500 nM, A3 > 1000 nM), displayed a favorable pharmacokinetic profile in preclinical species, and showed efficacy in functional in vitro models.

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Year:  2007        PMID： 17469811     DOI： 10.1021/jm061333v

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  11 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

2.  Homology modelling of the human adenosine A2B receptor based on X-ray structures of bovine rhodopsin, the beta2-adrenergic receptor and the human adenosine A2A receptor.

Authors:  Farag F Sherbiny; Anke C Schiedel; Astrid Maass; Christa E Müller
Journal:  J Comput Aided Mol Des       Date:  2009-11       Impact factor: 3.686

Review 3.  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

4.  Palladium-Catalyzed Coupling of Functionalized Primary and Secondary Amines with Aryl and Heteroaryl Halides: Two Ligands Suffice in Most Cases.

Authors:  Debabrata Maiti; Brett P Fors; Jaclyn L Henderson; Yoshinori Nakamura; Stephen L Buchwald
Journal:  Chem Sci       Date:  2011-01-01       Impact factor: 9.825

5.  New 2,6,9-trisubstituted adenines as adenosine receptor antagonists: a preliminary SAR profile.

Authors:  Catia Lambertucci; Gloria Cristalli; Diego Dal Ben; Dhuldeo D Kachare; Chiara Bolcato; Karl-Norbert Klotz; Giampiero Spalluto; Rosaria Volpini
Journal:  Purinergic Signal       Date:  2007-09-19       Impact factor: 3.765

6.  The Influence of the 1-(3-Trifluoromethyl-Benzyl)-1H-Pyrazole-4-yl Moiety on the Adenosine Receptors Affinity Profile of Pyrazolo[4,3-e][1,2,4]Triazolo[1,5-c]Pyrimidine Derivatives.

Authors:  Stephanie Federico; Sara Redenti; Mattia Sturlese; Antonella Ciancetta; Sonja Kachler; Karl-Norbert Klotz; Barbara Cacciari; Stefano Moro; Giampiero Spalluto
Journal:  PLoS One       Date:  2015-12-01       Impact factor: 3.240

7.  An electrochemical synthesis of functionalized arylpyrimidines from 4-amino-6-chloropyrimidines and aryl halides.

Authors:  Stéphane Sengmany; Erwan Le Gall; Eric Léonel
Journal:  Molecules       Date:  2011-06-29       Impact factor: 4.411

Review 8.  Therapeutic applications.

Authors:  Stephen Tilley; Jon Volmer; Maryse Picher
Journal:  Subcell Biochem       Date:  2011

9.  Progress in the discovery of selective, high affinity A(2B) adenosine receptor antagonists as clinical candidates.

Authors:  Rao V Kalla; Jeff Zablocki
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765

Review 10.  Exploration of chalcones and related heterocycle compounds as ligands of adenosine receptors: therapeutics development.

Authors:  Chrisna Matthee; Gisella Terre'Blanche; Lesetja J Legoabe; Helena D Janse van Rensburg
Journal:  Mol Divers       Date:  2021-06-27       Impact factor: 3.364
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