A New PqsR Inverse Agonist Potentiates Tobramycin Efficacy to Eradicate Pseudomonas aeruginosa Biofilms.

Autor: Schütz C; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.; Department of Pharmacy, Saarland University, Campus E8.1, Saarbrücken, 66123, Germany., Ho DK; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; Department of Pharmacy, Saarland University, Campus E8.1, Saarbrücken, 66123, Germany.; Department of Bioengineering, School of Medicine, University of Washington, Seattle, WA, 98195, USA., Hamed MM; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany., Abdelsamie AS; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.; Chemistry of Natural and Microbial Products Department, National Research Centre, Dokki, Cairo, 12622, Egypt., Röhrig T; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany., Herr C; Department of Internal Medicine V - Pulmonology, Allergology and Critical Care Medicine, Saarland University, Building 41, Homburg, 66421, Germany., Kany AM; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany., Rox K; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.; Department of Chemical Biology (CBIO), Helmholtz Centre for Infection Research (HZI), Inhoffenstr. 7, Braunschweig, 38124, Germany., Schmelz S; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.; Department of Structure and Function of Proteins (SFPR), Helmholtz Centre for Infection Research (HZI), Inhoffenstr. 7, Braunschweig, 38124, Germany., Siebenbürger L; PharmBioTec GmbH, Science Park 1, Saarbrücken, 66123, Germany., Wirth M; PharmBioTec GmbH, Science Park 1, Saarbrücken, 66123, Germany., Börger C; PharmBioTec GmbH, Science Park 1, Saarbrücken, 66123, Germany., Yahiaoui S; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany., Bals R; Department of Internal Medicine V - Pulmonology, Allergology and Critical Care Medicine, Saarland University, Building 41, Homburg, 66421, Germany., Scrima A; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.; Department of Structure and Function of Proteins (SFPR), Helmholtz Centre for Infection Research (HZI), Inhoffenstr. 7, Braunschweig, 38124, Germany., Blankenfeldt W; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.; Department of Structure and Function of Proteins (SFPR), Helmholtz Centre for Infection Research (HZI), Inhoffenstr. 7, Braunschweig, 38124, Germany., Horstmann JC; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; Department of Pharmacy, Saarland University, Campus E8.1, Saarbrücken, 66123, Germany., Christmann R; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; Department of Pharmacy, Saarland University, Campus E8.1, Saarbrücken, 66123, Germany., Murgia X; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; Gaiker Technology Centre, Zamudio, Bizkaia, 48170, Spain., Koch M; Leibniz Institute for New Materials, Campus D2.2, Saarbrücken, 66123, Germany., Berwanger A; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; Department of Pharmacy, Saarland University, Campus E8.1, Saarbrücken, 66123, Germany., Loretz B; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany., Hirsch AKH; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.; Department of Pharmacy, Saarland University, Campus E8.1, Saarbrücken, 66123, Germany., Hartmann RW; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.; Department of Pharmacy, Saarland University, Campus E8.1, Saarbrücken, 66123, Germany., Lehr CM; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; Department of Pharmacy, Saarland University, Campus E8.1, Saarbrücken, 66123, Germany., Empting M; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS)-Helmholtz Centre for Infection Research (HZI), Campus E8.1, Saarbrücken, 66123, Germany.; German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, Saarbrücken, 66123, Germany.; Department of Pharmacy, Saarland University, Campus E8.1, Saarbrücken, 66123, Germany.

Publikováno v: Advanced science (Weinheim, Baden-Wurttemberg, Germany) [Adv Sci (Weinh)] 2021 Jun; Vol. 8 (12), pp. e2004369. Date of Electronic Publication: 2021 Mar 18.

Cystobactamid 507: Concise Synthesis, Mode of Action, and Optimization toward More Potent Antibiotics.

Autor: Elgaher WAM; Department of Drug Design and Optimization, Helmholtz Institute for Pharmaceutical Research Saarland, Saarland University, Campus E8.1, 66123, Saarbrücken, Germany., Hamed MM; Department of Drug Design and Optimization, Helmholtz Institute for Pharmaceutical Research Saarland, Saarland University, Campus E8.1, 66123, Saarbrücken, Germany., Baumann S; Department of Microbial Natural Products, Helmholtz Institute for Pharmaceutical Research Saarland, Saarland University, Campus E8.1, 66123, Saarbrücken, Germany., Herrmann J; Department of Microbial Natural Products, Helmholtz Institute for Pharmaceutical Research Saarland, Saarland University, Campus E8.1, 66123, Saarbrücken, Germany., Siebenbürger L; PharmBioTec GmbH, 66123, Saarbrücken, Germany., Krull J; Department of Chemical Biology, Helmholtz Centre for Infection Research, Inhoffenstrasse 7, 38124, Braunschweig, Germany., Cirnski K; Department of Microbial Natural Products, Helmholtz Institute for Pharmaceutical Research Saarland, Saarland University, Campus E8.1, 66123, Saarbrücken, Germany., Kirschning A; Institute of Organic Chemistry, Leibniz University of Hannover, Schneiderberg 1B, 30167, Hannover, Germany., Brönstrup M; Department of Chemical Biology, Helmholtz Centre for Infection Research, Inhoffenstrasse 7, 38124, Braunschweig, Germany., Müller R; Department of Microbial Natural Products, Helmholtz Institute for Pharmaceutical Research Saarland, Saarland University, Campus E8.1, 66123, Saarbrücken, Germany., Hartmann RW; Department of Drug Design and Optimization, Helmholtz Institute for Pharmaceutical Research Saarland, Saarland University, Campus E8.1, 66123, Saarbrücken, Germany.

Publikováno v: Chemistry (Weinheim an der Bergstrasse, Germany) [Chemistry] 2020 Jun 05; Vol. 26 (32), pp. 7219-7225. Date of Electronic Publication: 2020 Apr 28.

Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis.

Autor: Abdelsamie AS; ElexoPharm GmbH , Im Stadtwald, Building A1.2 , 66123 Saarbrücken , Germany.; Chemistry of Natural and Microbial Products Department , National Research Centre , Dokki, 12622 Cairo , Egypt., Salah M; Department of Pharmaceutical and Medicinal Chemistry , Saarland University , 66123 Saarbrücken , Germany., Siebenbürger L; PharmBioTec GmbH , 66123 Saarbrücken , Germany., Merabet A; ElexoPharm GmbH , Im Stadtwald, Building A1.2 , 66123 Saarbrücken , Germany.; Institute of Pharmaceutical Chemistry , Philipps-University , 35032 Marburg , Germany., Scheuer C; Institute for Clinical & Experimental Surgery , Saarland University , 66421 Homburg/Saar , Germany., Frotscher M; Department of Pharmaceutical and Medicinal Chemistry , Saarland University , 66123 Saarbrücken , Germany., Müller ST; Institute for Zoology, Molecular Cell Physiology and Endocrinology , Technical University Dresden , 01062 Dresden , Germany., Zierau O; Institute for Zoology, Molecular Cell Physiology and Endocrinology , Technical University Dresden , 01062 Dresden , Germany., Vollmer G; Institute for Zoology, Molecular Cell Physiology and Endocrinology , Technical University Dresden , 01062 Dresden , Germany., Menger MD; Institute for Clinical & Experimental Surgery , Saarland University , 66421 Homburg/Saar , Germany., Laschke MW; Institute for Clinical & Experimental Surgery , Saarland University , 66421 Homburg/Saar , Germany., van Koppen CJ; ElexoPharm GmbH , Im Stadtwald, Building A1.2 , 66123 Saarbrücken , Germany.; Department of Pharmaceutical and Medicinal Chemistry , Saarland University , 66123 Saarbrücken , Germany., Marchais-Oberwinkler S; Institute of Pharmaceutical Chemistry , Philipps-University , 35032 Marburg , Germany., Hartmann RW; Department of Pharmaceutical and Medicinal Chemistry , Saarland University , 66123 Saarbrücken , Germany.; Department of Drug Design and Optimization , Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) , 66123 Saarbrücken , Germany.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2019 Aug 08; Vol. 62 (15), pp. 7289-7301. Date of Electronic Publication: 2019 Jul 25.

Human airway mucus alters susceptibility of Pseudomonas aeruginosa biofilms to tobramycin, but not colistin.

Autor: Müller L; Fraunhofer Institute for Toxicology and Experimental Medicine (Fraunhofer ITEM), Biomedical Research in Endstage and Obstructive Lung Disease Hannover (BREATH), Member of the German Centre for Lung Research (DZL), Member of the REBIRTH Cluster of Excellence, Nikolai-Fuchs-Straße 1, Hannover, Germany., Murgia X; Helmholtz Institute for Pharmaceutical Research (HIPS), Helmholtz Centre for Infection Research, Universitätscampus E8.1, Saarbrücken, Germany.; Korea Institute of Science and Technology, KIST Europe, Campus E7.1, Saarbrücken, Germany., Siebenbürger L; PharmBioTec GmbH, Science Park 1, Saarbrücken, Germany., Börger C; PharmBioTec GmbH, Science Park 1, Saarbrücken, Germany., Schwarzkopf K; Department of Anaesthesia and Intensive Care, Klinikum Saarbrücken, Winterberg 1, Saarbrücken, Germany., Sewald K; Fraunhofer Institute for Toxicology and Experimental Medicine (Fraunhofer ITEM), Biomedical Research in Endstage and Obstructive Lung Disease Hannover (BREATH), Member of the German Centre for Lung Research (DZL), Member of the REBIRTH Cluster of Excellence, Nikolai-Fuchs-Straße 1, Hannover, Germany., Häussler S; Helmholtz Institute for Infection Research, Inhoffenstraße 7, Braunschweig, Germany.; TWINCORE, Centre for Experimental and Clinical Infection Research, Feodor-Lynen-Straße 7, Hannover, Germany., Braun A; Fraunhofer Institute for Toxicology and Experimental Medicine (Fraunhofer ITEM), Biomedical Research in Endstage and Obstructive Lung Disease Hannover (BREATH), Member of the German Centre for Lung Research (DZL), Member of the REBIRTH Cluster of Excellence, Nikolai-Fuchs-Straße 1, Hannover, Germany., Lehr CM; Helmholtz Institute for Pharmaceutical Research (HIPS), Helmholtz Centre for Infection Research, Universitätscampus E8.1, Saarbrücken, Germany.; PharmBioTec GmbH, Science Park 1, Saarbrücken, Germany.; Department of Pharmacy, Saarland University, Campus, Saarbrücken, Germany., Hittinger M; PharmBioTec GmbH, Science Park 1, Saarbrücken, Germany., Wronski S; Fraunhofer Institute for Toxicology and Experimental Medicine (Fraunhofer ITEM), Biomedical Research in Endstage and Obstructive Lung Disease Hannover (BREATH), Member of the German Centre for Lung Research (DZL), Member of the REBIRTH Cluster of Excellence, Nikolai-Fuchs-Straße 1, Hannover, Germany.

Publikováno v: The Journal of antimicrobial chemotherapy [J Antimicrob Chemother] 2018 Oct 01; Vol. 73 (10), pp. 2762-2769.

Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC 50 for a proof-of-principle study.

Autor: Abdelsamie AS; Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany; Chemistry of Natural and Microbial Products Department, National Research Centre, Dokki, 12622 Cairo, Egypt., van Koppen CJ; ElexoPharm GmbH, Campus A12, D-66123 Saarbrücken, Germany., Bey E; ElexoPharm GmbH, Campus A12, D-66123 Saarbrücken, Germany., Salah M; Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany., Börger C; PharmBioTec GmbH, Science Park 1, D-66123 Saarbrücken, Germany., Siebenbürger L; PharmBioTec GmbH, Science Park 1, D-66123 Saarbrücken, Germany., Laschke MW; Institute for Clinical and Experimental Surgery, Saarland University, D-66421, Homburg/Saar, Germany., Menger MD; Institute for Clinical and Experimental Surgery, Saarland University, D-66421, Homburg/Saar, Germany., Frotscher M; Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany. Electronic address: m.frotscher@mx.uni-saarland.de.

Publikováno v: European journal of medicinal chemistry [Eur J Med Chem] 2017 Feb 15; Vol. 127, pp. 944-957. Date of Electronic Publication: 2016 Nov 04.