Indentification and optimisation of novel anti-infective agents using multiple hit-identification strategies

Publikacje

Evaluation of Bacterial RNA Polymerase Inhibitors in a Staphylococcus aureus -Based Wound Infection Model in SKH1 Mice

Autorzy: Jörg Haupenthal, Yannik Kautz, Walid A. M. Elgaher, Linda Pätzold, Teresa Röhrig, Matthias W. Laschke, Thomas Tschernig, Anna K. H. Hirsch, Vadim Molodtsov, Katsuhiko S. Murakami, Rolf W. Hartmann, Markus Bischoff
Opublikowane w: ACS Infectious Diseases, Numer 6/10, 2020, Strona(/y) 2573-2581, ISSN 2373-8227
Wydawca: American Chemical Society
DOI: 10.1021/acsinfecdis.0c00034

Protein‐Templated Hit Identification through an Ugi Four‐Component Reaction

Autorzy: Federica Mancini, M. Yagiz Unver, Walid A. M. Elgaher, Varsha R. Jumde, Alaa Alhayek, Peer Lukat, Jennifer Herrmann, Martin D. Witte, Matthias Köck, Wulf Blankenfeldt, Rolf Müller, Anna K. H. Hirsch
Opublikowane w: Chemistry – A European Journal, 2020, ISSN 0947-6539
Wydawca: John Wiley & Sons Ltd.
DOI: 10.1002/chem.202002250

From Wood to Tetrahydro-2-benzazepines in Three Waste-Free Steps: Modular Synthesis of Biologically Active Lignin-Derived Scaffolds

Autorzy: Saravanakumar Elangovan, Anastasiia Afanasenko, Jörg Haupenthal, Zhuohua Sun, Yongzhuang Liu, Anna K. H. Hirsch, Katalin Barta
Opublikowane w: ACS Central Science, Numer 5/10, 2019, Strona(/y) 1707-1716, ISSN 2374-7943
Wydawca: American Chemical Society
DOI: 10.1021/acscentsci.9b00781

Identification of RAD51–BRCA2 Inhibitors Using <i>N</i>-Acylhydrazone-Based Dynamic Combinatorial Chemistry

Autorzy: Greta Bagnolini; Beatrice Balboni; Fabrizio Schipani; Dario Gioia; Marina Veronesi; Francesca De Franco; Cansu Kaya; Ravindra P. Jumde; Jose Antonio Ortega; Stefania Girotto; Anna K. H. Hirsch; Marinella Roberti; Andrea Cavalli
Opublikowane w: ACS Med Chem Letters, Numer 1, 2022, ISSN 1948-5875
Wydawca: American Chemical Society
DOI: 10.1021/acsmedchemlett.2c00063

Discovery of Small-Molecule Stabilizers of 14-3-3 Protein–Protein Interactions via Dynamic Combinatorial Chemistry

Autorzy: Alwin M. Hartman, Walid A. M. Elgaher, Nathalie Hertrich, Sebastian A. Andrei, Christian Ottmann, Anna K. H. Hirsch
Opublikowane w: ACS Medicinal Chemistry Letters, Numer 11/5, 2020, Strona(/y) 1041-1046, ISSN 1948-5875
Wydawca: American Chemical Society
DOI: 10.1021/acsmedchemlett.9b00541

Rapid Discovery of Aspartyl Protease Inhibitors Using an Anchoring Approach

Autorzy: Markella Konstantinidou, Francesca Magari, Fandi Sutanto, Jörg Haupenthal, Varsha R. Jumde, M. Yagiz Ünver, Andreas Heine, Carlos Jamie Camacho, Anna K. H. Hirsch, Gerhard Klebe, Alexander Dömling
Opublikowane w: ChemMedChem, Numer 15/8, 2020, Strona(/y) 680-684, ISSN 1860-7179
Wydawca: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202000024

Design and Synthesis of Bioisosteres of Acylhydrazones as Stable Inhibitors of the Aspartic Protease Endothiapepsin

Autorzy: Varsha R. Jumde, Milon Mondal, Robin M. Gierse, M. Yagiz Unver, Francesca Magari, Roos C. W. van Lier, Andreas Heine, Gerhard Klebe, Anna K. H. Hirsch
Opublikowane w: ChemMedChem, Numer 13/21, 2018, Strona(/y) 2266-2270, ISSN 1860-7179
Wydawca: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.201800446

Potential Dental Biofilm Inhibitors: Dynamic Combinatorial Chemistry Affords Sugar‐Based Molecules that Target Bacterial Glucosyltransferase

Autorzy: Alwin M. Hartman, Varsha R. Jumde, Walid A. M. Elgaher, Evelien M. Te Poele, Lubbert Dijkhuizen, Anna K. H. Hirsch
Opublikowane w: ChemMedChem, 2020, ISSN 1860-7179
Wydawca: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202000222

N -Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting Pseudomonas aeruginosa Elastase and Clostridium Collagenases

Autorzy: Jelena Konstantinović, Samir Yahiaoui, Alaa Alhayek, Jörg Haupenthal, Esther Schönauer, Anastasia Andreas, Andreas M. Kany, Rolf Müller, Jesko Koehnke, Fabian K. Berger, Markus Bischoff, Rolf W. Hartmann, Hans Brandstetter, Anna K. H. Hirsch
Opublikowane w: Journal of Medicinal Chemistry, Numer 63/15, 2020, Strona(/y) 8359-8368, ISSN 0022-2623
Wydawca: American Chemical Society
DOI: 10.1021/acs.jmedchem.0c00584

Targeting the IspD Enzyme in the MEP Pathway: Identification of a Novel Fragment Class

Autorzy: Eleonora Diamanti; Mostafa M. Hamed; Antoine Lacour; Patricia Bravo; Boris Illarionov; Markus Fischer; Matthias Rottmann; Matthias Witschel; Anna K. H. Hirsch
Opublikowane w: ChemMedChem, Numer 6, 2022, ISSN 1860-7179
Wydawca: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202100679

"Phosphonate as a Stable Zinc-Binding Group for ""Pathoblocker"" Inhibitors of Clostridial Collagenase H (ColH)."

Autorzy: Katrin Voos; Esther Schönauer; Alaa Alhayek; Jörg Haupenthal; Anastasia Andreas; Rolf Müller; Rolf W. Hartmann; Hans Brandstetter; Anna K. H. Hirsch; Christian Ducho
Opublikowane w: Chemmedchem, Numer 1, 2021, ISSN 1860-7179
Wydawca: Wiley - V C H Verlag GmbbH & Co.
DOI: 10.1002/cmdc.202000994

Discovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases

Autorzy: Alaa Alhayek; Ahmed S. Abdelsamie; Esther Schönauer; Virgyl Camberlein; Evelyn Hutterer; Gernot Posselt; Jamil Serwanja; Constantin Blöchl; Christian G. Huber; Jörg Haupenthal; Hans Brandstetter; Silja Wessler; Anna K. H. Hirsch
Opublikowane w: J Med Chem, Numer 1, 2022, ISSN 0022-2623
Wydawca: American Chemical Society
DOI: 10.1021/acs.jmedchem.2c00785

Structure-Guided Optimization of Small-Molecule Folate Uptake Inhibitors Targeting the Energy-Coupling Factor Transporters

Autorzy: Alexander F. Kiefer, Spyridon Bousis, Mostafa M. Hamed, Eleonora Diamanti, Jörg Haupenthal, Anna K.H. Hirsch
Opublikowane w: Journal of Medicinal Chemistry, Numer 00222623, 2022, ISSN 0022-2623
Wydawca: American Chemical Society
DOI: 10.1021/acs.jmedchem.1c02114

Discovery of novel drug-like antitubercular hits targeting the MEP pathway enzyme DXPS by strategic application of ligand-based virtual screening.

Autorzy: Di Zhu; Sandra Johannsen; Tiziana Masini; Céline Simonin; Jörg Haupenthal; Boris Illarionov; Anastasia Andreas; Mahendra Awale; Robin M. Gierse; Tridia van der Laan; Ramon van der Vlag; Rita Nasti; Mael Poizat; Eric Buhler; Norbert Reiling; Rolf Müller; Markus Fischer; Jean-Louis Reymond; Anna K. H. Hirsch
Opublikowane w: Chemical Science, Numer 1, 2022, ISSN 2041-6539
Wydawca: Cambridge: Royal Society of Chemistry
DOI: 10.48350/174448

Flotillin-mediated membrane fluidity controls peptidoglycan synthesis and MreB movement.

Autorzy: Aleksandra Zielinska, Abigail Savietto, Anabela de Sousa Borges, Denis Martinez, Melanie Berbon, Joel R Roelofsen, Alwin M Hartman, Rinse de Boer, Ida J Van der Klei, Anna KH Hirsch, Birgit Habenstein, Marc Bramkamp, Dirk-Jan Scheffers
Opublikowane w: eLife, 2020, ISSN 2050-084X
Wydawca: eLife Sciences Publications
DOI: 10.7554/elife.57179

Hit-optimization using target-directed dynamic combinatorial chemistry: development of inhibitors of the anti-infective target 1-deoxy-d-xylulose-5-phosphate synthase

Autorzy: Ravindra P. Jumde, Melissa Guardigni, Robin M. Gierse, Alaa Alhayek, Di Zhu, Zhoor Hamid, Sandra Johannsen, Walid A. M. Elgaher, Philipp J. Neusens, Christian Nehls, Jörg Haupenthal, Norbert Reiling Anna K. H. Hirsch
Opublikowane w: Chemical Science, Numer 20416520, 2021, ISSN 2041-6520
Wydawca: Royal Society of Chemistry
DOI: 10.1039/d1sc00330e

Bacteriomimetic Liposomes Improve Antibiotic Activity of a Novel Energy-Coupling Factor Transporter Inhibitor

Autorzy: Menka Drost, Eleonora Diamanti, Kathrin Fuhrmann, Adriely Goes,Atanaz Shams, Jörg Haupenthal, Marcus Koch, Anna K. H. Hirsch, Gregor Fuhrmann
Opublikowane w: Pharmaceutics, Numer 19994923, 2022, ISSN 1999-4923
Wydawca: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/pharmaceutics14010004

Spray-drying of inhalable, multifunctional formulations for the treatment of biofilms formed in cystic fibrosis

Autorzy: Nashrawan Lababidi, Eric Ofosu Kissi, Walid A.M. Elgaher, Valentin Sigal, Jörg Haupenthal, Bianca C. Schwarz, Anna K.H. Hirsch, Thomas Rades, Marc Schneider
Opublikowane w: Journal of Controlled Release, Numer 314, 2019, Strona(/y) 62-71, ISSN 0168-3659
Wydawca: Elsevier BV
DOI: 10.1016/j.jconrel.2019.10.038

Energy-Coupling Factor Transporters as Novel Antimicrobial Targets

Autorzy: Spyridon Bousis, Inda Setyawati, Eleonora Diamanti, Dirk J. Slotboom, Anna K. H. Hirsch
Opublikowane w: Advanced Therapeutics, Numer 2/2, 2019, Strona(/y) 1800066, ISSN 2366-3987
Wydawca: WILEY-VCH
DOI: 10.1002/adtp.201800066

An Efficient Way to Screen Inhibitors of Energy-Coupling Factor (ECF) Transporters in a Bacterial Uptake Assay.

Autorzy: Spyridon Bousis; Steffen Winkler; Jörg Haupenthal; Francesco Fulco; Eleonora Diamanti; Anna K. H. Hirsch
Opublikowane w: International Journal of Molecular Sciences, Numer 3, 2022, ISSN 1422-0067
Wydawca: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ijms23052637

A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from d -galactose pentaacetate

Autorzy: Eva Zahorska, Sakonwan Kuhaudomlarp, Saverio Minervini, Sultaan Yousaf, Martin Lepsik, Thorsten Kinsinger, Anna K. H. Hirsch, Anne Imberty, Alexander Titz
Opublikowane w: Chemical Communications, Numer 56/62, 2020, Strona(/y) 8822-8825, ISSN 1359-7345
Wydawca: Royal Society of Chemistry
DOI: 10.1039/d0cc03490h

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