Literature DB >> 12540234

Ketones as building blocks for dynamic combinatorial libraries: highly active neuraminidase inhibitors generated via selection pressure of the biological target.

Matthias Hochgürtel1, Ralf Biesinger, Heiko Kroth, Dorothea Piecha, Michael W Hofmann, Sonja Krause, Otmar Schaaf, Claude Nicolau, Alexey V Eliseev.   

Abstract

New and potent inhibitors of neuraminidase, a key enzyme in the influenza virus activity, have been discovered in dynamic combinatorial libraries based on ketones and amines as building blocks. Selective synthesis of a number of inhibitors among multiple theoretically possible combinations of building blocks is driven by the presence of the target enzyme.

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Year:  2003        PMID: 12540234     DOI: 10.1021/jm025589m

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


  7 in total

1.  Direct screening of a dynamic combinatorial library using mass spectrometry.

Authors:  Sally-Ann Poulsen
Journal:  J Am Soc Mass Spectrom       Date:  2006-06-02       Impact factor: 3.109

2.  Interstrand DNA-DNA cross-link formation between adenine residues and abasic sites in duplex DNA.

Authors:  Nathan E Price; Kevin M Johnson; Jin Wang; Mostafa I Fekry; Yinsheng Wang; Kent S Gates
Journal:  J Am Chem Soc       Date:  2014-02-20       Impact factor: 15.419

3.  Design, preparation, and selection of DNA-encoded dynamic libraries.

Authors:  Gang Li; Wenlu Zheng; Zitian Chen; Yu Zhou; Yu Liu; Junrui Yang; Yanyi Huang; Xiaoyu Li
Journal:  Chem Sci       Date:  2015-09-11       Impact factor: 9.825

Review 4.  Protein-Directed Dynamic Combinatorial Chemistry: A Guide to Protein Ligand and Inhibitor Discovery.

Authors:  Renjie Huang; Ivanhoe K H Leung
Journal:  Molecules       Date:  2016-07-16       Impact factor: 4.411

5.  Optimized Inhibitors of MDM2 via an Attempted Protein-Templated Reductive Amination.

Authors:  Ramon van der Vlag; M Yagiz Unver; Tommaso Felicetti; Aleksandra Twarda-Clapa; Fatima Kassim; Cagdas Ermis; Constantinos G Neochoritis; Bogdan Musielak; Beata Labuzek; Alexander Dömling; Tad A Holak; Anna K H Hirsch
Journal:  ChemMedChem       Date:  2019-12-12       Impact factor: 3.466

6.  Discovery of potent inhibitors of human β-tryptase from pre-equilibrated dynamic combinatorial libraries.

Authors:  Qian-Qian Jiang; Wilhelm Sicking; Martin Ehlers; Carsten Schmuck
Journal:  Chem Sci       Date:  2014-12-08       Impact factor: 9.825

Review 7.  Dynamic template-assisted strategies in fragment-based drug discovery.

Authors:  Marco F Schmidt; Jörg Rademann
Journal:  Trends Biotechnol       Date:  2009-08-11       Impact factor: 19.536

  7 in total

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