A5090839909- Antimicrobial Peptides and Activities
- Antibiotic Resistance in Bacteria
- Bacterial biofilms and quorum sensing
- Asymmetric Hydrogenation and Catalysis
- Biochemical and Structural Characterization
- Catalytic C–H Functionalization Methods
- Quinazolinone synthesis and applications
- Pneumocystis jirovecii pneumonia detection and treatment
- Pneumonia and Respiratory Infections
- Bacteriophages and microbial interactions
- Click Chemistry and Applications
- Catalytic Alkyne Reactions
- Bacillus and Francisella bacterial research
- Oral microbiology and periodontitis research
Helmholtz Institute for Pharmaceutical Research Saarland
2022-2025
Helmholtz Centre for Infection Research
2022-2025
German Center for Infection Research
2025
Saarland University
2022-2025
Abstract Deriving active pharmaceutical agents from renewable resources is crucial to increasing the economic feasibility of modern biorefineries and promises alleviate critical supply‐chain dependencies in pharma manufacturing. Our multidisciplinary approach combines research lignin‐first biorefining, sustainable catalysis, alternative solvents with bioactivity screening, an vivo efficacy study, a structural‐similarity search. The resulting path novel anti‐infective, anti‐inflammatory,...
Abstract The ubiquitous opportunistic pathogen Pseudomonas aeruginosa is responsible for severe infections and notoriously known acquiring antimicrobial resistance. Inhibiting the bacterium's extracellular elastase, LasB – a zinc‐dependent protease presents promising strategy to mitigate its virulence. Within this medicinal chemistry–driven hit‐to‐lead optimization campaign, new series of highly potent dipeptidic phosphonates designed synthesized following structure–based drug‐discovery...
Antivirulence therapy has become a widely applicable method for fighting infections caused by multidrug-resistant bacteria. Among the many virulence factors produced Gram-negative bacterium Pseudomonas aeruginosa, elastase (LasB) stands out as an important target it plays pivotal role in invasion of host tissue and evasion immune response. In this work, we explored recently reported LasB inhibitor class α-benzyl-N-aryl mercaptoacetamides exploiting crystal structure one compounds. Our...
Infections caused by the Gram-negative pathogen Pseudomonas aeruginosa are emerging worldwide as a major threat to human health. Conventional antibiotic monotherapy suffers from rapid resistance development, underlining urgent need for novel treatment concepts. Here, we report on nontraditional approach combat P. aeruginosa-derived infections targeting its main virulence factor, elastase LasB. We discovered new chemical class of phosphonates with an outstanding in vitro ADMET and PK profile,...
Abstract Deriving active pharmaceutical agents from renewable resources is crucial to increasing the economic feasibility of modern biorefineries and promises alleviate critical supply‐chain dependencies in pharma manufacturing. Our multidisciplinary approach combines research lignin‐first biorefining, sustainable catalysis, alternative solvents with bioactivity screening, an vivo efficacy study, a structural‐similarity search. The resulting path novel anti‐infective, anti‐inflammatory,...
Despite the progress in surgical techniques and antibiotic prophylaxis, opportunistic wound infections with
Infections caused by the Gram-negative pathogen Pseudomonas aeruginosa are emerging worldwide as a major threat to human health. Conventional antibiotic monotherapy suffers from rapid resistance development, underlining urgent need for novel treatment concepts. Here, we report on non-traditional approach combat P. aeruginosa-derived infections targeting its main virulence factor, elastase LasB. We discovered new chemical class of phosphonates with an outstanding in vitro ADMET and PK...
The structural complexity of renewable resources offers remarkable opportunities for the environmentally friendly manufacturing essential pharmaceuticals, yet this has not been adequately addressed due to lack suitable methods. Our here described approach drug discovery, builds on innate features aromatic moiety lignin enable green pathways various classes biologically active molecules core dopamine structure. catalytic transformations are atom-economic, produce only harmless side-products...
Dual inhibitors of two key virulence factors Pseudomonas aeruginosa , the lectin LecA and protease LasB, open up an opportunity in current antimicrobial-resistance crisis.
The ubiquitous opportunistic pathogen Pseudomonas aeruginosa is responsible for severe infections and notoriously known acquiring antimicrobial resistance. Inhibiting the bacterium’s extracellular elastase, LasB – a zinc-dependent protease presents promising strategy to mitigate its virulence. Within this medicinal chemistry–driven hit-to-lead optimization campaign, new series of highly potent dipeptidic phosphonates designed synthesized following structure–based drug discovery approach. In...