Literature DB >> 20034791

A study of the effects of substituents on the selectivity of the binding of N-arylaminomethylene malonate inhibitors to DHODH.

Deborah Cowen1, Paul Bedingfield, Glenn A McConkey, Colin W G Fishwick, A Peter Johnson.   

Abstract

A series of mono- and di-substituted N-arylaminomethylene malonates have been used to probe the potential of utilizing additional H-bonding contacts in the ubiquinone binding channel, for selective inhibition between either human or Plasmodium DHODH. Altered 'head' group functionalities have been utilized in order to probe the role of specific functionalities within the inhibitors in terms of enzyme affinity and selectivity. Copyright (c) 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID: 20034791     DOI: 10.1016/j.bmcl.2009.11.079

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


  5 in total

1.  Conformational changes of the HsDHODH N-terminal Microdomain via DEER Spectroscopy.

Authors:  Eduardo F Vicente; Indra D Sahu; Antonio J Costa-Filho; Eduardo M Cilli; Gary A Lorigan
Journal:  J Phys Chem B       Date:  2015-07-02       Impact factor: 2.991

2.  De novo design of type II topoisomerase inhibitors as potential antimicrobial agents targeting a novel binding region.

Authors:  Kyle M Orritt; Lipeng Feng; Juliette F Newell; Jack N Sutton; Scott Grossman; Thomas Germe; Lauren R Abbott; Holly L Jackson; Benjamin K L Bury; Anthony Maxwell; Martin J McPhillie; Colin W G Fishwick
Journal:  RSC Med Chem       Date:  2022-06-16

3.  Structure-based ligand design of novel bacterial RNA polymerase inhibitors.

Authors:  Martin J McPhillie; Rachel Trowbridge; Katherine R Mariner; Alex J O'Neill; A Peter Johnson; Ian Chopra; Colin W G Fishwick
Journal:  ACS Med Chem Lett       Date:  2011-07-29       Impact factor: 4.345

4.  Expanding the Repertoire of Low-Molecular-Weight Pentafluorosulfanyl-Substituted Scaffolds.

Authors:  Arathy Jose; Daniel Guest; Remi LeGay; Graham J Tizzard; Simon J Coles; Mariliza Derveni; Edward Wright; Lester Marrison; Alpha A Lee; Aaron Morris; Matt Robinson; Frank von Delft; Daren Fearon; Lizbé Koekemoer; Tetiana Matviuk; Anthony Aimon; Christopher J Schofield; Tika R Malla; Nir London; Barnaby W Greenland; Mark C Bagley; John Spencer
Journal:  ChemMedChem       Date:  2022-02-22       Impact factor: 3.540

Review 5.  Driving antimalarial design through understanding of target mechanism.

Authors:  Petar P S Calic; Mahta Mansouri; Peter J Scammells; Sheena McGowan
Journal:  Biochem Soc Trans       Date:  2020-10-30       Impact factor: 5.407

  5 in total

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