Literature DB >> 18926700

Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.

Angel I Morales-Ramos1, John S Mecom, Terry J Kiesow, Todd L Graybill, Gregory D Brown, Nambi V Aiyar, Elizabeth A Davenport, Lorena A Kallal, Beth A Knapp-Reed, Peng Li, Allyn T Londregan, Dwight M Morrow, Shobha Senadhi, Reema K Thalji, Steve Zhao, Cynthia L Burns-Kurtis, Joseph P Marino.   

Abstract

High-throughput screening of the GSK compound collection against the P2Y(1) receptor identified a novel series of tetrahydro-4-quinolinamine antagonists. Optimal substitution around the piperidine group was pivotal for ensuring activity. An exemplar analog from this series was shown to inhibit platelet aggregation.

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Year:  2008        PMID: 18926700     DOI: 10.1016/j.bmcl.2008.09.102

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


  8 in total

Review 1.  P2Y nucleotide receptors: promise of therapeutic applications.

Authors:  Kenneth A Jacobson; Jean-Marie Boeynaems
Journal:  Drug Discov Today       Date:  2010-06-02       Impact factor: 7.851

2.  Pharmacochemistry of the platelet purinergic receptors.

Authors:  Kenneth A Jacobson; Francesca Deflorian; Shilpi Mishra; Stefano Costanzi
Journal:  Purinergic Signal       Date:  2011-02-18       Impact factor: 3.765

3.  Demystifying P2Y1 Receptor Ligand Recognition through Docking and Molecular Dynamics Analyses.

Authors:  Antonella Ciancetta; Robert D O'Connor; Silvia Paoletta; Kenneth A Jacobson
Journal:  J Chem Inf Model       Date:  2017-11-28       Impact factor: 4.956

4.  P2 receptors and platelet function.

Authors:  Béatrice Hechler; Christian Gachet
Journal:  Purinergic Signal       Date:  2011-07-27       Impact factor: 3.765

5.  Molecular Structure of P2Y Receptors: Mutagenesis, Modeling, and Chemical Probes.

Authors:  Kenneth A Jacobson; M P Suresh Jayasekara; Stefano Costanzi
Journal:  Wiley Interdiscip Rev Membr Transp Signal       Date:  2012-09-12

6.  Quinoline: A versatile heterocyclic.

Authors:  Akranth Marella; Om Prakash Tanwar; Rikta Saha; Mohammad Rahmat Ali; Sandeep Srivastava; Mymoona Akhter; Mohammad Shaquiquzzaman; Mohammad Mumtaz Alam
Journal:  Saudi Pharm J       Date:  2012-03-29       Impact factor: 4.330

7.  Virtual screening leads to the discovery of novel non-nucleotide P2Y₁ receptor antagonists.

Authors:  Stefano Costanzi; T Santhosh Kumar; Ramachandran Balasubramanian; T Kendall Harden; Kenneth A Jacobson
Journal:  Bioorg Med Chem       Date:  2012-07-03       Impact factor: 3.641

Review 8.  Update of P2Y receptor pharmacology: IUPHAR Review 27.

Authors:  Kenneth A Jacobson; Esmerilda G Delicado; Christian Gachet; Charles Kennedy; Ivar von Kügelgen; Beibei Li; M Teresa Miras-Portugal; Ivana Novak; Torsten Schöneberg; Raquel Perez-Sen; Doreen Thor; Beili Wu; Zhenlin Yang; Christa E Müller
Journal:  Br J Pharmacol       Date:  2020-04-06       Impact factor: 9.473

  8 in total

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