A5022978620- Cholinesterase and Neurodegenerative Diseases
- Parasitic infections in humans and animals
- Synthesis and Biological Evaluation
- Congenital Anomalies and Fetal Surgery
- Synthesis and biological activity
- Parasitic Infections and Diagnostics
- Alzheimer's disease research and treatments
- Amino Acid Enzymes and Metabolism
- Amoebic Infections and Treatments
- Biochemical and biochemical processes
- Phytochemistry and Biological Activities
- Cancer, Hypoxia, and Metabolism
- Plant chemical constituents analysis
- Glutathione Transferases and Polymorphisms
- Nanoparticle-Based Drug Delivery
- Chronic Obstructive Pulmonary Disease (COPD) Research
- Electrochemical sensors and biosensors
- Mass Spectrometry Techniques and Applications
- Computational Drug Discovery Methods
- Pharmacological Effects of Natural Compounds
- Biomedical Research and Pathophysiology
- Neonatal Health and Biochemistry
- Synthesis and Characterization of Heterocyclic Compounds
- Click Chemistry and Applications
- Advanced Drug Delivery Systems
Hacettepe University
2015-2025
Université Toulouse III - Paul Sabatier
2012
Institut des Maladies Métaboliques et Cardiovasculaires
2012
Inserm
2012
Abstract A series of (2 E )‐1‐(5‐bromothiophen‐2‐yl)‐3‐( para ‐substituted phenyl)prop‐2‐en‐1‐ones ( TB1 – TB11 ) was synthesized and tested for inhibitory activity toward human monoamine oxidase (hMAO). All compounds were found to be competitive, selective, reversible hMAO‐B except 2E )‐1‐(5‐bromothiophen‐2‐yl)‐3‐(4‐nitrophenyl)prop‐2‐en‐1‐one TB7 )‐1‐(5‐bromothiophen‐2‐yl)‐3‐(4‐chlorophenyl)prop‐2‐en‐1‐one TB8 ), which selective inhibitors hMAO‐A. The most potent compound,...
A series of 11 indole‐based chalcones ( IC1 – ) with various electron donating and withdrawing groups at the para position phenyl ring B were synthesized. All compounds tested for their human monoamine oxidase (hMAO)‐A hMAO‐B inhibitory potencies. Most synthesized candidates proved to be potent selective inhibitors MAO‐B rather than MAO‐A, a reversible competitive mode. Among them, compound IC9 was found inhibitor K i = 0.01 ± 0.005 μM selectivity index 120. It better standard drug,...
A series of new 2-methoxy-4-(5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)phenolderivatives, 4–13, were synthesized and tested for their human MAO inhibitory activity. All the compounds found to be selective reversible toward hMAO-A except 4, a inhibitor hMAO-B 12, nonselective inhibitor. Compound 7 was potent with Ki = 0.06 ± 0.003 μM having selectivity index (SI 1.02 × 10–5). It better than standard drug, Moclobemide (hMAO-A 0.11 0.01 μM) SI 0.049. Molecular docking simulation carried out...
Abstract Cystic Echinococcosis (CE) is a zoonotic disease caused by Echinococcus granulosus sensu lato. Diagnosing CE primarily relies on imaging techniques, and there crucial need for an objective laboratory test to enhance the diagnostic process. Today, cell-free DNAs (cfDNAs) have gained importance regarding their biomarker potential. This study aims investigate capabilities of different cfDNA targets (Echinococcus-specific repeat sequences (mgs-4 mgs-12) partial fragment repetitive...
Metabolite levels and turnover rates are necessary to understand metabolomic dynamics in a living organism fully. Amino acids can play distinct roles various cellular processes, their abnormal associated with pathological conditions, including cancer. Therefore, levels, especially rates, may provide enormous information about phenotype. 13C- or 13C,15N-labeled amino have also been commonly used trace acid metabolism. This study presented new methodology based on 18O labeling for that relied...
A series of thienylchalcones with fluoro and trifluoromethyl derivatives were synthesized evaluated for their capability to inhibit human monoamine oxidase B. The chemical structures the compounds have been ascertained by means 1HNMR, 13CNMR, mass spectroscopic data elemental analysis. results documented that these revealed moderate good inhibitory activities towards MAO-B than MAO-A. most active compound, (2E)-1-(thiophen-2-yl)-3-[4-(trifluoromethyl) phenyl] prop-2-en-1-one exhibited Ki...
For various neurodegenerative disorders like Alzheimer 's and Parkinson’ s diseases, selective reversible MAO ‐B inhibitors have a great therapeutic value. In our previous study, we shown that series of methoxylated chalcones with F functional group exhibited high binding affinity toward human monoamine oxidase‐B ( hMAO ‐B). continuation earlier study to extend the understanding structure–activity relationships, five new were studied for their inhibition . The results demonstrated these...
The inhibitory effects of flavonoids on monoamine oxidases (MAOs) have attracted great interest since alterations in monoaminergic transmission are reported to be related neurodegenerative diseases such as Parkinson’s and Alzheimer’s psychiatric disorders depression anxiety, thus MAOs may considered targets for the treatment these multi-factorial diseases. In present study, four Sideritis flavonoids, xanthomicrol (1), isoscutellarein...
This work aimed to evaluate the phenolic content and in vitro antioxidant, antimicrobial enzyme inhibitory activities of methanol extracts their fractions two edible halophytic Limonium species, L. effusum (LE) sinuatum (LS). The total resulted about two-fold higher ethyl acetate fraction LE (522.82 ± 5.67 mg GAE/g extract) than that LS (274.87 1.87 extract). LC-MS/MS analysis indicated tannic acid was most abundant both species (71,439.56 3643.3 µg/g extract 105,453.5 5328.1 LS), whereas...
Achilles tendon (AT) midsubstance injuries may heal suboptimally, especially in athletes. Transforming growth factor-beta 3 (TGF-β3) shows promise because of its recently discovered tendinogenic effects. Using poly(lactic-co-glycolic acid)-b-poly(ethylene glycol) (PLGA-b-PEG) nanoparticles (NPs) enhance the results by a sustained-release effect.The application TGF-β3 will AT healing, and NP form achieve better outcomes.Controlled laboratory study.A total 80 rats underwent unilateral...
Ferulic acid has structural similarity with curcumin which is being reported for its monoamine oxidase (MAO) inhibitory activity. Based on this similarity, we designed a series of ferulic amides 6a–m and tested their activity human MAO (hMAO) isoforms. All the compounds were found to inhibit hMAO isoforms either selectively or non‐selectively. Nine ( 6a , 6b 6g–m ) hMAO‐B selectively, whereas other four 6c – f be non‐selective. There gradual shift from selectivity b non‐selectivity as there...
A group of 3,5-diaryl-2-pyrazoline and hydrazone derivatives was prepared via the reaction various chalcones with hydrazide compounds in ethanol. Twenty original were synthesized. Ten these have a pyrazoline structure, nine one has chalcone structure. Structural elucidation performed by IR, (1)H NMR, (13)C mass spectral data, elemental analyses. These tested for their inhibitory activities toward B isoforms human monoamine oxidase (MAO). Except 3k 6c, all found to be competitive, reversible,...
Serotonin (5-HT) regulates different cardiac functions by acting directly on cardiomyocytes, fibroblasts and endothelial cells. Today, it is widely accepted that activated platelets represent a major source of 5-HT. In contrast, supposed production 5-HT in the heart still controversial. To address this issue, we investigated expression localization synthesizing enzyme tryptophan hydroxylase (TPH) L-aromatic amino acid decarboxylase (AADC) heart. We also evaluated their involvement TPH1 was...