A5000513924- Tryptophan and brain disorders
- Axial and Atropisomeric Chirality Synthesis
- Neural Networks Stability and Synchronization
- Phenothiazines and Benzothiazines Synthesis and Activities
- Neural Networks and Applications
- Analytical Chemistry and Chromatography
- Chemical Synthesis and Analysis
- Stress Responses and Cortisol
- Advanced Memory and Neural Computing
- Synthesis and Biological Activity
- Synthesis and Biological Evaluation
- Synthesis of Indole Derivatives
- Metal complexes synthesis and properties
- Multicomponent Synthesis of Heterocycles
- Asymmetric Synthesis and Catalysis
- Chemical Reaction Mechanisms
- Chemical synthesis and alkaloids
- Microwave-Assisted Synthesis and Applications
- Neuroinflammation and Neurodegeneration Mechanisms
- Molecular spectroscopy and chirality
- Neuroscience and Neuropharmacology Research
- Mass Spectrometry Techniques and Applications
- Crystallization and Solubility Studies
- Bioactive Compounds and Antitumor Agents
- Drug Transport and Resistance Mechanisms
University of Szeged
2016-2025
Hungarian Academy of Sciences
2013-2024
National Institute of Oncology
2022-2024
Országos Pszichiátriai és Neurológiai Intézet
2024
Research Network (United States)
2023
MTA-SZTE Research Group on Artificial Intelligence
2019
Institute for Computer Science and Control
2000-2010
University of Potsdam
2003-2009
Semmelweis University
2009
HUN-REN Institute for Nuclear Research
1997-2005
The central nervous system (CNS) is the final frontier in drug delivery because of blood-brain barrier (BBB), which poses significant barriers to access most drugs their targets. Kynurenic acid (KYNA), a tryptophan (Trp) metabolite, plays an important role behavioral functions and abnormal KYNA levels have been observed neuropsychiatric conditions. current challenge lies delivering CNS owing its polar side chain. Recently, C-3 chain modified analogs shown cross BBB; however, it unclear...
The central nervous system (CNS) is the final frontier in drug delivery because of blood–brain barrier (BBB), which poses significant barriers to access most drugs their targets. Kynurenic acid (KYNA), a tryptophan (Trp) metabolite, plays an important role behavioral functions, and abnormal KYNA levels have been observed neuropsychiatric conditions. current challenge lies delivering CNS owing its polar side chain. Recently, C-3 chain-modified analogs shown cross BBB; however, it unclear...
A recently proposed strategy to overcome multidrug resistance (MDR) in cancer is target the collateral sensitivity of otherwise resistant cells. We designed a library 120 compounds explore chemical space around previously identified 8-hydroxyquinoline-derived Mannich bases with robust MDR-selective toxicity. included study effect halogen and alkoxymethyl substitutions R5 combination different R7, shift base from R7 R5, as well introduction an aromatic moiety. Cytotoxicity tests performed on...
The syntheses and transformations of 1-(α-aminobenzyl)-2-naphthol (Betti base) derivatives are reviewed. Special attention is paid to the applications enantiopure Betti base as chiral ligands in asymmetric transformations. Keywords: aminonaphthols, betti base, naphthoxazines, tautomerism
Background: Quinoline-derived metabolites exhibit notable chemical complexity. What causes minor structural alterations to induce significant changes in disease outcomes? Historically eclipsed by more straightforward scaffolds, these chemicals provide a dynamic nexus tryptophan metabolism, connecting immunomodulation, excitotoxicity, and cancer. However, they often fail at the blood–brain barrier, we currently lack understanding of how specific influence bioavailability off-target effects....
Abstract By means of simple or domino ring‐closure reactions 1‐(α‐aminobenzyl)‐2‐naphthol (Betti base: 1 ), 1‐aminomethyl‐2‐naphthol (2) and 2‐(α‐aminobenzyl)‐1‐naphthol (reverse Betti 3 ) with phosgene, ethyl benzimidate, 2‐carboxybenzaldehyde, levulinic acid, salicylaldehyde/formalin salicylaldehyde/acetaldehyde, naphth[1,2‐ e ][1,3]oxazine naphth[2,1‐ derivatives were prepared. All the nitrogen‐bridged polycyclic containing a number centers asymmetry formed nearly complete...
A relationship between p<italic>K</italic><sub>a</sub> values, binding abilities to copper(<sc>ii</sc>) and iron(<sc>iii</sc>) anticancer activity of 8-hydroxyquinoline derived Mannich bases.
Purpose: The investigation of anti-inflammatory and immunosuppressive functions Kynurenic acid (KYNA) is now in focus. There also substantial evidence that TSG-6 has an activity. Therefore, the present study, we compared effects newly synthetized KYNA analogues on TNF-α production U-937 monocytic cells correlation with expression. Methods: was measured by ELISA, expression determined RTqPCR method. As cytokine inducers Staphylococcus aureus Chlamydia pneumoniae were used. Results: attenuated...
Background and Aims The systemic host response in sepsis is frequently accompanied by central nervous system (CNS) dysfunction. Evidence suggests that excessive formation of neutrophil extracellular traps (NETs) can increase the permeability blood–brain barrier (BBB) evolving mitochondrial damage may contribute to pathogenesis sepsis-associated encephalopathy. Kynurenic acid (KYNA), a metabolite tryptophan catabolism, exerts pleiotropic cell-protective effects under pro-inflammatory...
The disubstitution effects of X and Y in 1-(Y-phenyl)-3-(X-phenyl)-2,3-dihydro-1H-naphth[1,2-e][1,3]oxazines on the ring-chain tautomerism, delocalization nitrogen lone pair (anomeric effect), (13)C NMR chemical shifts were analyzed by using multiple linear regression analysis. Study three-component equilibrium B<==>A<==>C revealed that chain<==>trans (A<==>B) constants are significantly influenced inductive effect (sigma(F)) substituent 1-phenyl ring. In contrast, no significant dependence...
The multidrug resistance (MDR) proteins are present in a majority of human tumours. Their activity is important to understand the chemotherapeutic failure. A search for MDR-reversing compounds was conducted among various Betti-base derivatives tylosin. Here, we evaluate vitro and vivo P-glycoprotein (P-gp)-modulating most promising compound N-tylosil-1-α-amino-(3-bromophenyl)-methyl-2-naphthol (TBN) using MDR1 gene-transfected parental L5178 mouse lymphoma cell lines. In experiments showed...
Vascular adhesion protein-1 (VAP-1) is a primary amine oxidase and drug target for inflammatory vascular diseases. Despite extensive attempts to develop potent, specific, reversible inhibitors of its enzyme activity, the task has proven challenging. Here we report synthesis, inhibitory molecular binding mode novel pyridazinone inhibitors, which show specificity VAP-1 over monoamine diamine oxidases. The crystal structures three inhibitor-VAP-1 complexes that these compounds bind reversibly...
Synthesis and characterization of an 8-hydroxyquinoline–proline hybrid, its complex formation with half-sandwich organometallic cations: aqueous chemistry, lipophilicity, cellular uptake anticancer activity.
Multidrug resistance (MDR) in cancer is one of the major obstacles chemotherapy. We have recently identified a series 8-hydroxyquinoline Mannich base derivatives with MDR-selective toxicity, however limited solubility. In this work, novel 5-nitro-8-hydroxyquinoline-proline hybrid and its Rh(η5-C5Me5) Ru(η6-p-cymene) complexes excellent aqueous solubility were developed, characterized, tested against sensitive MDR cells. Complex formation ligand essential metal ions was also investigated...
Abstract We previously showed the anti-inflammatory effects of kynurenic acid (KYNA) and its brain-penetrable analog N -(2-(dimethylamino)ethyl)-3-(morpholinomethyl)-4-hydroxyquinoline-2-carboxamide (SZR104) both in vivo vitro. Here, we identified cytomorphological KYNA SZR104 secondary microglial cultures established from newborn rat forebrains. quantitatively analyzed selected morphological aspects microglia control (unchallenged), lipopolysaccharide (LPS)-treated (challenged), KYNA- or...