A5045285658- Chemical Synthesis and Analysis
- Phenothiazines and Benzothiazines Synthesis and Activities
- Quinazolinone synthesis and applications
- Asymmetric Hydrogenation and Catalysis
- Innovative Microfluidic and Catalytic Techniques Innovation
- Synthesis and biological activity
- Photochromic and Fluorescence Chemistry
- Luminescence and Fluorescent Materials
- Synthesis and Catalytic Reactions
- Nanoparticle-Based Drug Delivery
- Supramolecular Self-Assembly in Materials
- Synthesis and Biological Evaluation
- Carbon dioxide utilization in catalysis
- Nanoplatforms for cancer theranostics
- Catalytic C–H Functionalization Methods
- Biochemical and Molecular Research
- Synthesis of β-Lactam Compounds
- Flavonoids in Medical Research
- Biological Activity of Diterpenoids and Biflavonoids
- Catalytic Cross-Coupling Reactions
- Cancer therapeutics and mechanisms
- Asymmetric Synthesis and Catalysis
- Sulfur Compounds in Biology
- Microbial metabolism and enzyme function
- Carbon and Quantum Dots Applications
Semmelweis University
2015-2025
Institute of Materials and Environmental Chemistry
2018-2024
HUN-REN Research Centre for Natural Sciences
2018-2024
Institute of Organic Chemistry
2024
Abstract Baicalin is a flavone glycoside extracted from Scutellaria baicalensis , traditional Chinese herbal medicine. Numerous pharmacological effects of baicalin were reported ( e.g. antioxidant, anxiolytic); nevertheless, the most important physicochemical properties influencing pharmacokinetic behaviour and concomitant oral bioavailability have not yet been described in comprehensive study. The aim this project was to characterize acid-base, lipophilicity, biorelevant solubility...
Abstract Semicarbazide-sensitive amine oxidase (SSAO) catalyses oxidative deamination of primary amines. Since there is no data about its function in pain and arthritis mechanisms, we investigated the effects our novel SSAO inhibitor SzV-1287 chronic mouse models joint inflammation. Effects (20 mg/kg i.p./day) were K/BxN serum-transfer complete Freund’s adjuvant (CFA)-evoked active immunization compared to reference LJP-1207. Mechanonociception was assessed by aesthesiometry, oedema...
Central nervous system (CNS) tumors are exceptionally difficult to treat, and oxidative stress-inducing radiotherapy is an important treatment modality. In this study, we examined self-assembling pro-drug nanoconjugates of naturally derived antitumor ecdysteroids, which were designed interfere with stress in brain tumor cells. Eight ecdysteroid-squalene conjugates semi-synthesized formulated into self-assembled aqueous nanosuspensions, showed excellent stability for up 16 weeks. The...
The Suzuki-Miyaura reaction is one of the most used transformations in drug research. Thus making this more sustainable considerable current interest. Here we show that propylene carbonate (PC) can be as a solvent for reaction. PC greenest solvents since it synthesized under green conditions by use carbon dioxide air. All reactions proceeded well and good or excellent yields were observed biaryl products. Nonetheless case pyridazinones, 2-hydroxypropyl- chain containing side-products...
Enantiodiscriminative helix formation was observed for β-peptide H14 helices. This observation is caused by the synperiplanar orientation of H-O atoms which more unfavorable than those H-H interaction. The 1,2 interaction leads to destruction helical structure. introduction a double C-C bond in backbone rules out formation.
Inspired by the 8-dimethylaminoquinoline (8-DMAQ) caging chromophore, photocleavable 8-aminoquinoline derivatives were prepared with aim of furnishing a robust synthetic pathway for novel cage scaffolds. The four-step versatile process allows facile introduction various amino-substituents and its overall yield is feasible scale-up. photocages showed high photolysis efficiency low fluorescence, comparable to literature reference compounds (as 8-DMAQ-OAc, BHQ-OAc CyHQ-OAc), demonstrating...
Abstract Carbonized polymer dots (CPDs), a peculiar type of carbon dots, show extremely high quantum yields, making them very attractive nanostructures for application in optics and biophotonics. The origin the strong photoluminescence CPDs resides complicated interplay several radiative mechanisms. To understand correlation between CPD processing properties, early stage formation carbonized has been studied. In synthesis, citric acid monohydrate 2‐amino‐2‐(hydroxymethyl)propane‐1,3‐diol...
SZV 1287 is our novel multi-target analgesic, which seems to be a promising drug candidate for the treatment of neuropathic pain. Therefore, development process has been started in 2016. Since pharmacokinetic characterization essential and albumin binding drugs can strongly affect their properties, herein we provided detailed investigation interaction its known metabolites with serum albumin. In preliminary animal study, demonstrated appearance 1287, oxaprozin, L 2799, 2805, 2811 circulation...
Abstract Comparative synthesis of some new quinazoline derivatives via tetrakis(triphenylphosphine)palladium(0) catalysed Suzuki‐Miyaura cross‐coupling reaction in “green” propylene carbonate (PC) and dimethoxyethane. Three haloquinazolines were synthesised for Suzuki‐cross‐coupling from 5‐bromoanthranilic acid. Sufficient easy method the elimination PC is developed, thus optimization was carried out. Reactions with 2‐chloro‐6‐bromo‐3‐phenylquinazolin‐4(3 H )‐one proceeded faster a higher...
Cyclizations of 2-(2-vinyl)phenoxy- tert -anilines under thermal conditions yield oxazonine or octahydro-dipyrroloquinoline products. The transformations can be considered as further extensions [1, n ]-H transfer and cyclization tertiary anilines.
The imbalance between prooxidants and antioxidants in biological systems, known as oxidative stress, can lead to a disruption of redox signaling by the reactive oxygen/nitrogen species is related severe diseases. most vulnerable moiety targeted oxidant pathways thiol (SH) group cysteine residues, especially its deprotonated (S − ) form. Cysteine, along with oxidized, disulfide-containing form, cystine, constitute one abundant low molecular weight couples, providing significant contribution...
8-Aminoquinolines are useful molecular motifs for ion sensors.To encourage chemosensor development, new building blocks containing these essential.8-Aminoquinoline-2-carbaldehydes proposed as since their aldehyde group offers the possibility further transformations.We present a general method preparation of compounds starting from commercially available 8-bromo-2methylquinoline. Different sidechains fine-tuning affinity and selectivity were introduced by microwave-aided N-arylation using...
Self-assembled peptide nanostructures with stimuli-responsive features are promising as functional materials. Despite extensive research efforts, water-soluble supramolecular constructs that can interact lipid membranes in a controllable way still challenging to achieve. Here, we have employed short membrane anchor protein motif (GLFD) and coupled it spiropyran photoswitch. Under physiological conditions, these conjugates assemble into ∼3.5 nm thick, foil-like bilayer morphologies....
Self-assembling peptides offer a versatile set of tools for bottom-up construction supramolecular biomaterials. Among these compounds, non-natural peptidic foldamers experience increased focus due to their structural variability and lower sensitivity enzymatic degradation. However, very little is known about membrane properties complex oligomeric assemblies - key areas biomedical technological applications. Here we designed short, acyclic β3-peptide sequences with alternating amino acid...
Several ecdysteroid acetonides act as adjuvant chemo-sensitizing agents against various cancer cell lines, and they can be formulated to self-assembling nanoparticle (NP) pro-drugs through a hydrolysable conjugation with squalene. In the bloodstream such squalenoylated nanoparticles dissolve into low-density lipoprotein (LDL) that allows targeting tissues containing high levels of LDL-receptors. this work, ajugasterone C 2,3;20,22-diacetonide (3) 11α-hydroxypoststerone 2,3-acetonide (4) were...
Abstract Oxindole is a widely used scaffold in drug discovery, which can be found several marketed drugs, among them sunitinib and ziprasidone. Thus, the derivatization of oxindole considerable current interest. The extreme reaction conditions (high temperature, high pressure) described literature for batchwise regioselective multistep 3-alkylation with alcohols presence Raney nickel motivated us to develop robust, time- cost-efficient continuous-flow variant this reaction. In addition,...
A new, eco-friendly process utilising the green solvent propylene carbonate (PC) has been developed to perform
Four fused nitrogen-containing ring systems were investigated by electrospray ionization-tandem mass spectrometry: Pyridazino-indoles, pyridazino-quinolines, a pyrimido-quinoline derivative and pyrimido-cinnolines. Fragmentation patterns of these compounds are discussed compared. Several characteristic cross-ring fragments formed mainly on the pyridazine pyrimidine rings systems. The connected Cl, NO2 , Me, Ph more extended heterocyclic substituents influenced fragmentation.
Abstract Herein we report the synthesis of a set novel N -benzoylthioureas, 2-(acyl)amino-4 H -3,1-benzothiazin-4-ones and thiourea derivatives with amino acid moieties. The corresponding benzoyl isothiocyanates were synthesised from variety substituted chlorides ammonium thiocyanate or benzoic acids trichloroisocyanuric acid/triphenylphosphine (TCCA/TPP) system. resulting compounds reacted substances containing groups to give new molecules functionalities, which could be potential chloride...