Literature DB >> 23806553

Discovery of triazines as potent, selective and orally active PDE4 inhibitors.

Rainer Gewald1, Christian Grunwald, Ute Egerland.   

Abstract

Expanding on HTS hit 4 afforded a series of [1,3,5]triazine derivatives as novel PDE4 inhibitors. The SAR development and optimization process with the emphasis on ligand efficiency and physicochemical properties led to the discovery of compound 44 as a potent, selective and orally active PDE4 inhibitor.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID： 23806553     DOI： 10.1016/j.bmcl.2013.05.099

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


  6 in total

1.  Pharmacophore modeling, 3D-QSAR, and docking study of pyrozolo[1,5-a]pyridine/4,4-dimethylpyrazolone analogues as PDE4 selective inhibitors.

Authors:  Naga Srinivas Tripuraneni; Mohammed Afzal Azam
Journal:  J Mol Model       Date:  2015-10-26       Impact factor: 1.810

2.  Discovery of triazines as selective PDE4B versus PDE4D inhibitors.

Authors:  Timothy J Hagen; Xuesheng Mo; Alex B Burgin; David Fox; Zheng Zhang; Mark E Gurney
Journal:  Bioorg Med Chem Lett       Date:  2014-06-12       Impact factor: 2.823

3.  A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein.

Authors:  Marius S Pop; Nicolas Stransky; Colin W Garvie; Jean-Philippe Theurillat; Emily C Hartman; Timothy A Lewis; Cheng Zhong; Elizabeth K Culyba; Fallon Lin; Douglas S Daniels; Raymond Pagliarini; Lucienne Ronco; Angela N Koehler; Levi A Garraway
Journal:  Mol Cancer Ther       Date:  2014-04-15       Impact factor: 6.261

4.  Surface Binding Energy Landscapes Affect Phosphodiesterase Isoform-Specific Inhibitor Selectivity.

Authors:  Qing Liu; Andreas Herrmann; Qiang Huang
Journal:  Comput Struct Biotechnol J       Date:  2018-12-28       Impact factor: 7.271

5.  Long-Timescale Simulations Revealed Critical Non-Conserved Residues of Phosphodiesterases Affecting Selectivity of BAY60-7550.

Authors:  Qing Liu; Menghua Song; Yue Qiu; Elaine Lai-Han Leung; Qiang Huang; Xiaojun Yao
Journal:  Comput Struct Biotechnol J       Date:  2022-09-13       Impact factor: 6.155

6.  Synthesis, Pharmacological Profile and Docking Studies of New Sulfonamides Designed as Phosphodiesterase-4 Inhibitors.

Authors:  Isabelle Karine da Costa Nunes; Everton Tenório de Souza; Suzana Vanessa S Cardozo; Vinicius de Frias Carvalho; Nelilma Correia Romeiro; Patrícia Machado Rodrigues E Silva; Marco Aurélio Martins; Eliezer J Barreiro; Lídia Moreira Lima
Journal:  PLoS One       Date:  2016-10-03       Impact factor: 3.240
  6 in total

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