Literature DB >> 23356879

Synthesis and structure-activity relationship studies of novel dual inhibitors of soluble epoxide hydrolase and 5-lipoxygenase.

Karin Meirer1, Carmen B Rödl, Joanna M Wisniewska, Sven George, Ann-Kathrin Häfner, Estel-la Buscató, Franca-Maria Klingler, Steffen Hahn, Dirk Berressem, Sandra K Wittmann, Dieter Steinhilber, Bettina Hofmann, Ewgenij Proschak.   

Abstract

Current research leads to the assumption that drugs affecting more than one target could result in a more efficient treatment of diseases and fewer safety concerns. Administration of drugs inhibiting only one branch of the arachidonic acid cascade is usually accompanied by side effects. We therefore designed and synthesized a library of hybrid molecules incorporating an imidazo[1,2-a]pyridine and an urea moiety as novel soluble epoxide hydrolase (sEH)/5-lipoxygenase (5-LO) dual inhibitors. Evaluation of the compounds was accomplished by in vitro testing using recombinant enzyme assays.

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Year:  2013        PMID: 23356879     DOI: 10.1021/jm301617j

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


  10 in total

1.  Exploring the chemical space of multitarget ligands using aligned self-organizing maps.

Authors:  Janosch Achenbach; Franca-Maria Klingler; René Blöcher; Daniel Moser; Ann-Kathrin Häfner; Carmen B Rödl; Simon Kretschmer; Björn Krüger; Frank Löhr; Holger Stark; Bettina Hofmann; Dieter Steinhilber; Ewgenij Proschak
Journal:  ACS Med Chem Lett       Date:  2013-10-23       Impact factor: 4.345

Review 2.  Cytochrome P450 epoxygenase pathway of polyunsaturated fatty acid metabolism.

Authors:  Arthur A Spector; Hee-Yong Kim
Journal:  Biochim Biophys Acta       Date:  2014-08-02

Review 3.  The 2014 Bernard B. Brodie award lecture-epoxide hydrolases: drug metabolism to therapeutics for chronic pain.

Authors:  Sean D Kodani; Bruce D Hammock
Journal:  Drug Metab Dispos       Date:  2015-03-11       Impact factor: 3.922

Review 4.  Development of multitarget agents possessing soluble epoxide hydrolase inhibitory activity.

Authors:  Kerstin Hiesinger; Karen M Wagner; Bruce D Hammock; Ewgenij Proschak; Sung Hee Hwang
Journal:  Prostaglandins Other Lipid Mediat       Date:  2018-12-26       Impact factor: 3.072

5.  Pharmacological profile and efficiency in vivo of diflapolin, the first dual inhibitor of 5-lipoxygenase-activating protein and soluble epoxide hydrolase.

Authors:  Ulrike Garscha; Erik Romp; Simona Pace; Antonietta Rossi; Veronika Temml; Daniela Schuster; Stefanie König; Jana Gerstmeier; Stefanie Liening; Markus Werner; Heiner Atze; Sandra Wittmann; Christina Weinigel; Silke Rummler; Gerhard K Scriba; Lidia Sautebin; Oliver Werz
Journal:  Sci Rep       Date:  2017-08-24       Impact factor: 4.379

6.  Discovery of the first dual inhibitor of the 5-lipoxygenase-activating protein and soluble epoxide hydrolase using pharmacophore-based virtual screening.

Authors:  Veronika Temml; Ulrike Garscha; Erik Romp; Gregor Schubert; Jana Gerstmeier; Zsofia Kutil; Barbara Matuszczak; Birgit Waltenberger; Hermann Stuppner; Oliver Werz; Daniela Schuster
Journal:  Sci Rep       Date:  2017-02-20       Impact factor: 4.379

7.  Design, Synthesis and Cellular Characterization of a Dual Inhibitor of 5-Lipoxygenase and Soluble Epoxide Hydrolase.

Authors:  Karin Meirer; Daniel Glatzel; Simon Kretschmer; Sandra K Wittmann; Markus Hartmann; René Blöcher; Carlo Angioni; Gerd Geisslinger; Dieter Steinhilber; Bettina Hofmann; Robert Fürst; Ewgenij Proschak
Journal:  Molecules       Date:  2016-12-29       Impact factor: 4.411

8.  Systematic Assessment of Fragment Identification for Multitarget Drug Design.

Authors:  Steffen Brunst; Jan S Kramer; Whitney Kilu; Jan Heering; Julius Pollinger; Kerstin Hiesinger; Sven George; Dieter Steinhilber; Daniel Merk; Ewgenij Proschak
Journal:  ChemMedChem       Date:  2021-02-04       Impact factor: 3.466

Review 9.  Small Molecule Soluble Epoxide Hydrolase Inhibitors in Multitarget and Combination Therapies for Inflammation and Cancer.

Authors:  Amarjyoti Das Mahapatra; Rinku Choubey; Bhaskar Datta
Journal:  Molecules       Date:  2020-11-24       Impact factor: 4.411

Review 10.  Discovery of Soluble Epoxide Hydrolase Inhibitors from Chemical Synthesis and Natural Products.

Authors:  Cheng-Peng Sun; Xin-Yue Zhang; Christophe Morisseau; Sung Hee Hwang; Zhan-Jun Zhang; Bruce D Hammock; Xiao-Chi Ma
Journal:  J Med Chem       Date:  2020-12-28       Impact factor: 7.446

  10 in total

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