Literature DB >> 16143532

SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors.

Johann Leban1, Martin Kralik, Jan Mies, Michael Gassen, Karin Tentschert, Roland Baumgartner.   

Abstract

Novel DHODH inhibitors were developed based on a previously described series by introduction of heteroatoms into the cyclopentene ring and hydroxyl groups attached to it. Also, the hydrophobic biphenyl side chain was replaced with benzyloxy phenyl groups. Activities on human, rat, and mouse enzymes indicate a species specificity of these inhibitors.

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Year:  2005        PMID: 16143532     DOI: 10.1016/j.bmcl.2005.07.053

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


  7 in total

1.  4SC-101, a novel small molecule dihydroorotate dehydrogenase inhibitor, suppresses systemic lupus erythematosus in MRL-(Fas)lpr mice.

Authors:  Onkar P Kulkarni; Sufyan G Sayyed; Claudia Kantner; Mi Ryu; Max Schnurr; Miklós Sárdy; Johann Leban; Ruediger Jankowsky; Aldo Ammendola; Robert Doblhofer; Hans-Joachim Anders
Journal:  Am J Pathol       Date:  2010-04-22       Impact factor: 4.307

Review 2.  DHODH and cancer: promising prospects to be explored.

Authors:  Yue Zhou; Lei Tao; Xia Zhou; Zeping Zuo; Jin Gong; Xiaocong Liu; Yang Zhou; Chunqi Liu; Na Sang; Huan Liu; Jiao Zou; Kun Gou; Xiaowei Yang; Yinglan Zhao
Journal:  Cancer Metab       Date:  2021-05-10

3.  Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH).

Authors:  Marianne Lucas-Hourani; Hélène Munier-Lehmann; Farah El Mazouni; Nicholas A Malmquist; Jane Harpon; Eloi P Coutant; Sandrine Guillou; Olivier Helynck; Anne Noel; Artur Scherf; Margaret A Phillips; Frédéric Tangy; Pierre-Olivier Vidalain; Yves L Janin
Journal:  J Med Chem       Date:  2015-06-30       Impact factor: 7.446

4.  Repositioning an Immunomodulatory Drug Vidofludimus as a Farnesoid X Receptor Modulator With Therapeutic Effects on NAFLD.

Authors:  Yanlin Zhu; Shuangshuang Xu; Yi Lu; Yijuan Wei; Benqiang Yao; Fusheng Guo; Xing Zheng; Yumeng Wang; Ying He; Lihua Jin; Yong Li
Journal:  Front Pharmacol       Date:  2020-05-14       Impact factor: 5.810

5.  IMU-838, a Developmental DHODH Inhibitor in Phase II for Autoimmune Disease, Shows Anti-SARS-CoV-2 and Broad-Spectrum Antiviral Efficacy In Vitro.

Authors:  Friedrich Hahn; Christina Wangen; Sigrun Häge; Antonia Sophia Peter; Gerhard Dobler; Brett Hurst; Justin Julander; Jonas Fuchs; Zsolt Ruzsics; Klaus Überla; Hans-Martin Jäck; Roger Ptak; Andreas Muehler; Manfred Gröppel; Daniel Vitt; Evelyn Peelen; Hella Kohlhof; Manfred Marschall
Journal:  Viruses       Date:  2020-12-05       Impact factor: 5.048

6.  TNFα-induced metabolic reprogramming drives an intrinsic anti-viral state.

Authors:  Jessica Ciesla; Isreal Moreno; Joshua Munger
Journal:  PLoS Pathog       Date:  2022-07-14       Impact factor: 7.464

7.  Novel Dihydroorotate Dehydrogenase Inhibitors with Potent Interferon-Independent Antiviral Activity against Mammarenaviruses In Vitro.

Authors:  Yu-Jin Kim; Beatrice Cubitt; Yingyun Cai; Jens H Kuhn; Daniel Vitt; Hella Kohlhof; Juan C de la Torre
Journal:  Viruses       Date:  2020-07-29       Impact factor: 5.048

  7 in total

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