Literature DB >> 21507636

A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor.

Peter Bach1, Jonas Boström, Kay Brickmann, J J J van Giezen, Ragnar Hovland, Annika U Petersson, Asim Ray, Fredrik Zetterberg.   

Abstract

A novel series of P2Y(12) antagonists for development of drugs within the antiplatelet area is presented. The synthesis of the piperazinyl-pyridine urea derivatives and their structure-activity relationships (SAR) are described. Several compounds showed P2Y(12) antagonistic activities in the sub-micromolar range.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21507636     DOI: 10.1016/j.bmcl.2011.03.088

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


  3 in total

1.  Potentiation of TRAP-6-induced platelet dense granule release by blockade of P2Y12 signaling with MRS2395.

Authors:  Annachiara Mitrugno; Rachel A Rigg; Nicole B Laschober; Anh T P Ngo; Jiaqing Pang; Craig D Williams; Joseph E Aslan; Owen J T McCarty
Journal:  Platelets       Date:  2017-05-19       Impact factor: 3.862

2.  Modeling ligand recognition at the P2Y12 receptor in light of X-ray structural information.

Authors:  Silvia Paoletta; Davide Sabbadin; Ivar von Kügelgen; Sonja Hinz; Vsevolod Katritch; Kristina Hoffmann; Aliaa Abdelrahman; Jens Straßburger; Younis Baqi; Qiang Zhao; Raymond C Stevens; Stefano Moro; Christa E Müller; Kenneth A Jacobson
Journal:  J Comput Aided Mol Des       Date:  2015-07-21       Impact factor: 3.686

3.  Novel Thienopyrimidine-Based PET Tracers for P2Y12 Receptor Imaging in the Brain.

Authors:  Berend van der Wildt; Bieneke Janssen; Aleksandra Pekošak; E Johanna L Stéen; Robert C Schuit; Esther J M Kooijman; Wissam Beaino; Danielle J Vugts; Albert D Windhorst
Journal:  ACS Chem Neurosci       Date:  2021-11-10       Impact factor: 4.418

  3 in total

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