A5004304720- Bioactive Compounds and Antitumor Agents
- Carbohydrate Chemistry and Synthesis
- Cancer therapeutics and mechanisms
- Synthesis and biological activity
- Natural Compound Pharmacology Studies
- Microbial Natural Products and Biosynthesis
- Chemical Synthesis and Analysis
- Polysaccharides and Plant Cell Walls
- Multicomponent Synthesis of Heterocycles
- Plant biochemistry and biosynthesis
- Synthesis of Organic Compounds
- Circadian rhythm and melatonin
- Sleep and related disorders
- Ion Channels and Receptors
- Phytochemicals and Antioxidant Activities
- Computational Drug Discovery Methods
- Sleep and Wakefulness Research
- Click Chemistry and Applications
- Acute Lymphoblastic Leukemia research
TU Dresden
2024
University of Stuttgart
2017-2023
Friedrich-Alexander-Universität Erlangen-Nürnberg
2020
Orexins are neuropeptides that activate the rhodopsin-like G protein-coupled receptors OX1R and OX2R. The orexin system plays an important role in regulation of sleep-wake cycle feeding emotions. nonselective receptor antagonist suvorexant has been first drug on market targeting is prescribed for treatment insomnia. Subtype-selective antagonists valuable tools to further investigate functions physiological vivo promising lead compounds addiction, anxiety, pain or obesity. Starting from OX2R...
Abstract In the past 20 years, peptide‐based antibiotics, such as vancomycin, teicoplanin, and daptomycin, have often been considered second‐line antibiotics. However, in recent an increasing number of reports on vancomycin resistance pathogens appeared, which forces researchers to find novel lead structures for potent new Herein, we report total synthesis a defined endo‐type B PPAP library their antibiotic activity against multiresistant S. aureus various vancomycin‐resistant Enterococci ....
Recently, a series of endo-type B polycyclic polyprenylated acylphloroglucinols (PPAP) derivatives with high antimicrobial activities were chemically synthesized. One the derivatives, PPAP 23, which showed activity and low cytotoxicity, was chosen for further investigation its bactericidal profiles mode action. 23 better efficacy in killing methicillin resistant S. aureus (MRSA) decreasing metabolic 5-day-old biofilm cells than vancomycin. Moreover, did not appear to develop resistance...
In response to the pressing global challenge of antibiotic resistance, time efficient design and synthesis novel antibiotics are immense need. Polycyclic polyprenylated acylphloroglucinols (PPAP) were previously reported effectively combat a range gram-positive bacteria. Although exact mode action is still not clear, we conceptualized late-stage divergent approach expand our natural product-based PPAP library by 30 additional entities perform SAR studies against methicillin-resistant...
Polycyclic polyprenylated acylphloroglucinols (PPAPs) comprise a large group of compounds mostly plant origin. The best-known compound is hyperforin from St. John's wort with its antidepressant, antitumor and antimicrobial properties. Chemical synthesis PPAP variants allows the generation improved activity compatibility. Here we studied two synthetic PPAP-derivatives, 23 53, as to their activity. While insoluble in water, sodium salt, water-soluble. In vitro, both exhibited good...
Pre-SARS-CoV-2, tuberculosis was the leading cause of death by a single pathogen. Repetitive exposure Mycobacterium tuberculosis(Mtb) supported development multidrug- and extensively drug-resistant strains, demanding novel drugs. Hyperforin, natural type A polyprenylated polycyclic acylphloroglucinol from St. John's wort, exhibits antidepressant antibacterial effects also against Mtb. Yet, Hyperforin's instability limits utility in clinical practice. Here, we present photo- bench-stable B...
Selective modulation of TRPC6 ion channels is a promising therapeutic approach for neurodegenerative diseases and depression. A significant advancement showcases the selective activation through metalated type-B PPAP, termed PPAP53. This success stems from PPAP53's 1,3-diketone motif facilitating metal coordination. PPAP53 water-soluble as potent hyperforin, gold standard in this field. In contrast to type-A, PPAPs offer advantages such gram-scale synthesis, easy derivatization, long-term...
Abstract In den vergangenen 20 Jahren wurden peptidbasierte Antibiotika wie Vancomycin, Teicoplanin oder Daptomycin als Reserveantibiotika betrachtet. letzten erschienen jedoch vermehrt Berichte über Vancomycin‐resistente Krankheitserreger, was die Entwicklung neuartiger Leitstrukturen für neue wirksame motivierte. Hier wird Totalsynthese einer definierten endo‐Typ‐B‐PPAP‐Bibliothek und deren antibiotische Aktivität gegen multiresistente Staphylococcus‐aureus‐ diverse Enterococcus‐Stämme...
Polycyclic polyprenylated acylphloroglucinols (PPAPs) comprise a large group of compounds mostly plant origin. The best-known compound is hyperforin from St. John's wort with its antidepressant, antitumor and antimicrobial properties. chemical synthesis PPAP variants allows the generation improved activity compatibility. Here, we studied two synthetic PPAP-derivatives, water-insoluble PPAP23 water-soluble sodium salt PPAP53. In vitro, both exhibited good against methicillin-resistant
Before the emergence of SARS-CoV-2, tuberculosis (TB) was leading cause infectious disease mortality worldwide. Like all antibiotic-exposed bacteria Mycobacterium (Mtb) developed multidrug-resistant (MDR) and exten-sively drug-resistant (XDR) strains which require new antibiotics with novel mechanism actions. Hyperforin, a natural type-A polyprenylated polycyclic acylphloroglucinol (PPAP) isolated from St. John’s wort, is known for its antibacterial, antidepressant antimycobacterial...
Before the emergence of SARS-CoV-2, tuberculosis (TB) was leading cause infectious disease mortality worldwide. Like all antibiotic-exposed bacteria Mycobacterium (Mtb) developed multidrug-resistant (MDR) and exten-sively drug-resistant (XDR) strains which require new antibiotics with novel mechanism actions. Hyperforin, a natural type-A polyprenylated polycyclic acylphloroglucinol (PPAP) isolated from St. John’s wort, is known for its antibacterial, antidepressant antimycobacterial...
The selective modulation of TRPC6 ion channels has emerged as a promising therapeutic approach for treating neuro-degenerative diseases and depression. Here, we present significant advancement in this field by demonstrating the se-lective activation using metallated type-B PPAP, designated PPAP53. success PPAP53 is attributed to utilization 1,3-diketone motif PPAPs metal coordination. exhibit water solubility equipotent activity compared hyperforin, which natural product considered gold...
Before the emergence of SARS-CoV-2, tuberculosis (TB) was leading cause infectious disease mortality worldwide. Like all antibiotic-exposed bacteria Mycobacterium (Mtb) developed multidrug-resistant (MDR) and exten-sively drug-resistant (XDR) strains which require new antibiotics with novel mechanism actions. Hyperforin, a natural type-A polyprenylated polycyclic acylphloroglucinol (PPAP) isolated from St. John’s wort, is known for its antibacterial, antidepressant antimycobacterial...