A5087817896- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
- Synthesis of heterocyclic compounds
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Reactions of Organic Compounds
- Quinazolinone synthesis and applications
- Synthesis and biological activity
- Phenothiazines and Benzothiazines Synthesis and Activities
- Fluorine in Organic Chemistry
- Synthesis and Reactivity of Heterocycles
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Pharmacological Receptor Mechanisms and Effects
- Asymmetric Synthesis and Catalysis
- Receptor Mechanisms and Signaling
- Chemical Reaction Mechanisms
- Synthesis and Catalytic Reactions
- Analytical Chemistry and Chromatography
- Cancer therapeutics and mechanisms
- Crystallography and molecular interactions
- Coordination Chemistry and Organometallics
- Organic and Inorganic Chemical Reactions
- Synthesis and Reactivity of Sulfur-Containing Compounds
Gdańsk Medical University
2016-2025
University of Gdańsk
2015-2018
Georgia State University
2008-2015
The University of Texas Medical Branch at Galveston
2013
A series of quaternary ammonium fluoroquinolones was obtained by exhaustive methylation the amine groups present at 7-position fluoroquinolones, including ciprofloxacin, enoxacin, gatifloxacin, lomefloxacin, and norfloxacin. The synthesized molecules were tested for their antibacterial antibiofilm activities against Gram-positive Gram-negative human pathogens, i.e. Staphylococcus aureus Pseudomonas aeruginosa. study showed that compounds are potent agents (MIC values lowest 6.25 μM) with low...
This review provides a comprehensive overview of recent advancements in the design and synthesis biologically active quaternary ammonium compounds (QACs). The covered scope extends beyond commonly reviewed antimicrobial derivatives to include synthetic agents with antifungal, anticancer, antiviral properties. Additionally, this highlights examples exhibiting activity against protozoa herbicidal effects, as well analgesic anesthetic derivatives. article also embraces...
Abstract magnified image The addition reaction of lithium reagents to the 4 position 2‐chloropyrimidine or 2‐chloroquinazoline followed by oxidation resultant dihydro intermediate product is a powerful tool for synthesis 4‐substituted 2‐chloropyrimidines 2‐chloroquinazolines. 4‐Vinyl derivatives undergo conjugate nucleophilic across vinyl group. A displacement chloride in 2‐chloroquinazolines treatment with 4‐methylpiperazine provides compounds that are antagonists serotonin 5‐HT 2A...
Fluorescent labeling utilizing Cu(I)-catalyzed azide–alkyne cycloaddition reactions (CuAAC) is among the leading applications of “click” chemistry strategy. probes for this approach can be constructed by linking an azide or alkyne group to a fluorophore, such as recently developed Safirinium derivatives. These compounds are water-soluble, highly fluorescent heterocycles based on 1,2,4-triazolium, with significant potential various applications, although they have not yet been converted...
Lipophilicity is a vital physicochemical parameter of molecule, which affects several biological processes such as absorption, tissue distribution, and pharmacokinetic properties. In this study, evaluation lipophilicities series novel fluoroquinolone-Safirinium dye hybrids using chromatographic computational methods presented. Fluoroquinolone-Safirinium have been synthesized new dual-acting hydrophilic antibacterial agents. Reversed phase thin-layer chromatography micellar electrokinetic...
A series of 2-imino-2H-chromen-3-yl-1,3,5-triazine compounds 5⁻12, which are namely hybrids 2,4-diamino-1,3,5-triazines and 2-imino-coumarins, was synthesized by reacting 2-(4,6-diamine-1,3,5-triazin-2-yl)acetonitriles 1⁻4 with 2-hydroxybenzaldehydes. After this, upon heating in aqueous DMF, 2-imino-2H-chromen-3-yl-1,3,5-triazines 10 12 were converted into the corresponding 2H-chromen-3-yl-1,3,5-triazines 13 14, essentially coumarins. The vitro anticancer activity newly prepared evaluated...
This study investigates the antibacterial N-heterocyclic carbene (NHC)–silver complexes using SwissADME platform, a web-based tool developed by Swiss Institute of Bioinformatics (SIB). NHCs, particularly their silver complexes, have gained significant interest in medicinal chemistry for potential as and anticancer agents. The effectiveness these is closely linked to structure, including factors like lipophilicity, which enhance ability penetrate bacterial cells sustain release active ions....
The lipophilicity of a molecule is well-recognized as crucial physicochemical factor that conditions the biological activity drug candidate. This study was aimed to evaluate isoxazolo[3,4-b]pyridine-3(1H)-ones and their N1-substituted derivatives, which demonstrated pronounced antifungal activities. Several methods, including reversed-phase thin layer chromatography (RP-TLC), reversed phase high-performance liquid (RP-HPLC), micellar electrokinetic (MEKC), were employed. Furthermore,...
Tandem fluorogenic reaction: A new platform for the direct, selective and sensitive detection of formaldehyde and/or secondary aliphatic amines, based on a tandem Mannich–electrophilic amination reaction, is described. Biological applications hydrophilic, water-soluble fluorescent 2,2-dialkyl-2,3-dihydro-[1,2,4]triazolo[4,3-a]pyridin-2-ium-8-carboxylates (Safarinium P probes) are exemplified by labeling amine-containing Ac-AKF-NH2 peptide Bacillus subtilis spores in aqueous solution. As...
2-hydroxylamino-4,5-dihydroimidazolium-O-sulfonate (1) has been prepared by reacting 2-chloro-4,5-dihydroimidazole with hydroxylamine-O-sulfonic acid. Deprotonated compound 1a containing both the nucleophilic endocyclic nitrogen atoms and electrophilic exocyclic was used for syntheses of 3-substituted 6,7-dihydro-5H-imidazo[2,1-c][1,2,4]oxadiazoles 2-9 6,7-dihydro-5H-imidazo[2,1-c][1,2,4]thiadiazole-3-thione (10) tandem addition-electrophilic amination reaction. The method promises utility...
Abstract 2‐Aryl(arylsulfonyl)‐6,7‐dihydro‐2 H ‐imidazo[2,1‐ c ][1,2,4]triazol‐3(5 )‐ones and 3‐arylimino‐6,7‐dihydroimidazo[2,1‐ ][1,2,4]thiadiazoles have been synthesized by intramolecular nucleophilic substitution reactions at the electron‐deficient sp 2 nitrogen atom of 2‐(hydroxyimino)imidazolidine O ‐sulfonate. The displacement sulfate leaving group both sulfur anionic nucleophiles proceeds exothermically in‐plane S N 2σ substitution.
We have used isoxazolo[3,4-b]pyridin-3(1H)-one and isoxazolo[3,4-b]quinolin-3(1H)-one as "masked" heterocyclic hydroxylamines to generate Paal-Knorr intermediates of the Trofimov pyrrole synthesis. The previously inaccessible intermediates, trapped by ethyl propiolate, were obtained reacting corresponding isoxazolones with 4-fold excess propiolate under basic conditions at ambient temperature, characterized means IR NMR spectroscopic data well single crystal X-ray analysis. Quantum chemical...
Currently, rapid evaluation of the physicochemical parameters drug candidates, such as lipophilicity, is in high demand owing to it enabling approximation processes absorption, distribution, metabolism, and elimination. Although lipophilicity candidates determined using shake flash method (
Proteinogenic amino acids were derivatized via coupling reactions with N-hydroxysuccinimide esters of Safirinium dyes. The obtained compounds fully characterized by 1H and 13C NMR, IR, ESI-MS spectral techniques. Elemental analysis, as well the crystal structure analysis exemplary compounds, performed. absorption fluorescent properties derivatives have been systematically investigated. optical very good water solubility allowed for development a simple method determination means micellar...