Drug Design and Optimization

This group is located at the Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)

 

In order to combat the increasing number of resistant pathogens, the development of new antibiotic drugs is an important goal for pharmaceutical research. Lacking in this field are efficient medications that fight infectious diseases. As a result, scientists are constructing and improving novel agents that target essential processes in bacteria. This is done with the aim of killing or attenuating these pathogens. Below, you may read more about the optimization of new drug candidates.

Complete List of Publications of DDOP (Rolf W. Hartmann)

Download the complete List of Publications

Selected Publications

Lu, C., Maurer, C.K., Kirsch, B., Steinbach, A., Hartmann, R.W. (2014) Overcoming unexpected functional inversion of PqsR antagonist in Pseudomonas aeruginosa led to the first in vivo potent anti-virulence agent targeting pqs quorum sensing, Angewandte, 53, 1109 –1112

Storz, M.P., Brengel, C., Weidel, E.,  Hoffmann, M., Hollemeyer, K., Empting, M. Steinbach, A., Müller, R., Hartmann, R.W. (2013) Biochemical and biophysical analysis of a chiral PqsD inhibitor revealing tight-binding behavior and enantiomers with contrary thermodynamic signatures, ACS Chem. Biol., 8, 2794-2801

Sahner, H.J., Brengel, C.,  Storz, Groh, M., Plaza, A.P.,  Negri, M.,  Müller, R., Hartmann, R.W. (2013) Combining in silico and biophysical methods for the development of Pseudomonas aeruginosa quorum sensing inhibitors - an alternative approach for structure-based drug design, J. Med.Chem., 56, 8656-8664

Zender, M., Klein, T., Henn, C., Kirsch, B., Maurer, C.K., Kail, D., Ritter, C., Dolezal, O., Steinbach, A., Hartmann, R.W.(2013) Discovery and Biophysical Characterization of 2-Amino-Oxadiazoles as novel Antagonists of PqsR - an important regulator of Pseudomonas aeruginosa virulence, J. Med. Chem., 56, 6761−6774

Weidel, E., DeJong, J., Brengel, C., Storz, M., Braunshausen, A., Negri, M., Plaza, A., Steinbach, A., Müller, R., Hartmann, R. (2013) Structure Optimization of 2-Benzamidobenzoic acids as PqsD inhibitors for Pseudomonas aeruginosa infections and elucidation of binding mode by SPR, STD NMR and molecular docking, J. Med. Chem., 56, 6146−6155

Hüsecken, K., Negri, M., Fruth, M., Hartmann, R.W., Haupenthal, J. (2013) Peptide-based investigation of the Escherichia coli RNA polymerase σ70:core interface as target site, ACS Chem. Biol., 8, 758–766

Storz,M.P.; Maurer,C.K.; Zimmer,C.; Wagner,N.; Brengel,C.; De Jong,J.C.; Lucas,S.; Musken,M.; Häußler,Susanne; Steinbach,A.; Hartmann,Rolf W.;  (Jahr: 2012). Titel: Validation of PqsD as an Anti-biofilm Target in Pseudomonas aeruginosa by Development of Small-Molecule Inhibitors. Zeitschrift: Journal of the American Chemical Society

Leader

  • Prof Dr Rolf W. Hartmann

    Rolf Hartmann

    Head of the Department Drug Design and Optimization

    +49 681 98806-2000

    + 49 681 98806-2009

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Audio Podcast

  • Kündigung für Biofilm-WGs – Pharmazeuten des HIPS stören Bakteriengemeinschaften
    Bakterien haben einen ausgeprägten Gemeinschaftssinn und verschanzen sich gerne in schleimigen Biofilmen. Etwa 60 Prozent aller bakteriellen Infektionen lösen inzwischen Biofilme aus. Ein besonders geselliger Keim ist Pseudomonas aeruginosa. Er ist besonders für Mukoviszidose-Patienten gefährlich. Wissenschaftler am Helmholtz-Institut für Pharmazeutische Forschung Saarland suchen nach Wegen, seine Biofilme aufzulösen – damit Medikamente wirken können. Begleiten Sie Anke Steinbach in Ihre Labore...