59 hasil untuk "Gabriel Marc"
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Artikel Jurnal Teks lengkap
Design, Synthesis and Evaluation of Antioxidant and NSAID Derivatives with Antioxidant, Anti-Inflammatory and Plasma Lipid Lowering Effects
Amides containing methyl esters of γ-aminobutyric acid (GABA), L-proline and L-tyrosine, and esters containing 3-(pyridin-3-yl)propan-1-ol were synthesized by conjugation with 3,5-di-tert-butyl-4-hydroxybenzoic, an NSAID (tolfenamic acid), or 3-phenylacrylic (cinnamic…
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Structure–Activity Relationship Studies Based on Quinazoline Derivatives as EGFR Kinase Inhibitors (2017–Present)
The epidermal growth factor receptor (EGFR) plays a critical role in the tumorigenesis of various forms of cancer. Targeting the mutant forms of EGFR has been identified as an attractive therapeutic approach and led to the approval of three generations of inhibitors. The quinazoline core has…
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Exploring the Inhibitory Potential of Phytosterols β-Sitosterol, Stigmasterol, and Campesterol on 5-Alpha Reductase Activity in the Human Prostate: An In Vitro and In Silico Approach
Steroidal 5α-reductase type 2 (S5αR2) is a key enzyme involved in the conversion of testosterone (TST) to dihydrotestosterone (DHT), a crucial process in the development of benign prostatic hyperplasia (BPH). Phytosterols (PSs), natural plant-derived compounds, have been proposed as potential…
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Artikel Jurnal Teks lengkap
New Phenolic Derivatives of Thiazolidine-2,4-dione with Antioxidant and Antiradical Properties: Synthesis, Characterization, In Vitro Evaluation, and Quantum Studies
Oxidative stress has been incriminated in the physiopathology of many diseases, such as diabetes, cancer, atherosclerosis, and cardiovascular and neurodegenerative diseases. There is a great interest in developing new antioxidants that could be useful for preventing and treating conditions for…
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In Silico Evaluation of Some Computer-Designed Fluoroquinolone–Glutamic Acid Hybrids as Potential Topoisomerase II Inhibitors with Anti-Cancer Effect
Background/Objectives: Fluoroquinolones (FQs) are topoisomerase II inhibitors with antibacterial activity, repositioned recently as anti-cancer agents. Glutamic acid (GLA) is an amino acid that affects human metabolism. Since an anti-cancer mechanism of FQs is human topoisomerase II inhibition, it…
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N-(4-Methoxyphenethyl)-2-propylpentanamide
Herein, we report the mechanochemical synthesis of a novel hybrid molecule, N-(4-methoxyphenethyl)-2-propylpentanamide. This solvent-minimized synthesis aligns with the principles of Green Chemistry and exemplifies the emerging paradigm of medicinal mechanochemistry, offering an efficient…
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Ethyl 2-(2-((6-Methyl-4-oxo-4H-chromen-3-yl)methylene)hydrazineyl)thiazole-4-carboxylate
This study presents the synthesis of a new compound, ethyl 2-(2-((6-methyl-4-oxo-4H-chromen-3-yl)methylene)hydrazinyl)thiazole-4-carboxylate, obtained by the Hantzsch heterocyclisation reaction. The compound was analyzed through melting point determination, 1H and 13C NMR spectroscopy, infrared…
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Inclusion of a Catechol-Derived Hydrazinyl-Thiazole (CHT) in β-Cyclodextrin Nanocavity and Its Effect on Antioxidant Activity: A Calorimetric, Spectroscopic and Molecular Docking Approach
The aim of the present research was to obtain a supramolecular complex between a strong antioxidant compound previously reported by our group, in order to extend its antioxidant activity. The formation of the inclusion complex of a catechol hydrazinyl-thiazole derivative (CHT) and β-cyclodextrin in…
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ANTIOXIDANT ACTIVITY AND DFT STUDIES OF ETHYL 2-(2-((6-METHYL-4-OXO-4H-CHROMEN-3-YL) METHYLENE)HYDRAZINYL)THIAZOLE-4-CARBOXYLATE
ABSTRACT. The microwave-assisted improved synthesis of ethyl 2-(2-((6-methyl-4-oxo-4H-chromen-3-yl)methylene)hydrazinyl)thiazole-4-carboxylate is described. The antioxidant potential of the target compound was evaluated using spectrophotometric methods, including the DPPH• and ABTS•⁺ radical…
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An Overview of the Structure–Activity Relationship in Novel Antimicrobial Thiazoles Clubbed with Various Heterocycles (2017–2023)
Antimicrobial resistance is an increasing problem for global public health. One of the strategies to combat this issue is the synthesis of novel antimicrobials through rational drug design based on extensive structure–activity relationship studies. The thiazole nucleus is a prominent feature in the…
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Antioxidant activity and antibacterial evaluation of new thiazolin-4-one derivatives as potential tryptophanyl-tRNA synthetase inhibitors
The rapid emergence of bacterial resistance to antibiotics currently available for treating infectious diseases requires effective antimicrobial agents with new structural profiles and mechanisms of action. Twenty-three thiazolin-4-one derivatives were evaluated for their antibacterial activity by…
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Badnaviruses and banana genomes: a long association sheds light on Musa phylogeny and origin
Badnaviruses are double‐stranded DNA pararetroviruses of the family Caulimoviridae. Badnaviral sequences found in banana are distributed over three main clades of the genus Badnavirus and exhibit wide genetic diversity. Interestingly, the nuclear genome of many plants, including banana, is invaded…
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Trimetazidine–Profen Hybrid Molecules: Synthesis, Chemical Characterization, and Biological Evaluation of Their Racemates
Background: Trimetazidine is a clinically established cardioprotective agent with anti-ischemic and antioxidant properties, widely used in the management of coronary artery disease. Combining its metabolic and cytoprotective effects with the potent anti-inflammatory activity of profens presents a…
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Mechanochemical Synthesis of Valproic Acid-Based Hybrids: Antioxidant, Anti-Inflammatory, and In Silico Evaluation
Valproic acid is a clinically important therapeutic agent whose biological properties have stimulated the development of structurally modified derivatives with improved pharmacological profiles. In the present study, nine amino–valproic acid hybrids were synthesized by a rapid mechanochemical…
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New Antioxidant Triphenol-Derived Hydrazide-Hydrazone Thiazole: Formation and Analysis of Inclusion Complex with β-CD Using Experimental and Computational Approaches
A new water-soluble not-colored antioxidant (Z)-N′-(4-(3,4-dihydroxyphenyl)-3-ethylthiazol-2(3H)-ylidene)-4-hydroxybenzohydrazide hydrochloride (DHTH) was obtained and characterized. The interaction between DHTH and β-CD was studied by experimental thermodynamic methods such as isothermal titration…
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Novel Flurbiprofen Derivatives as Antioxidant and Anti-Inflammatory Agents: Synthesis, In Silico, and In Vitro Biological Evaluation
In this study, we present the synthesis of five novel compounds by combining flurbiprofen with various substituted 2-phenethylamines. The synthesized derivatives underwent comprehensive characterization using techniques such as 1H- and 13C-NMR spectroscopy, UV-Vis spectroscopy, and high-resolution…
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An Insight into Rational Drug Design: The Development of In-House Azole Compounds with Antimicrobial Activity
Antimicrobial resistance poses a major threat to global health as the number of efficient antimicrobials decreases and the number of resistant pathogens rises. Our research group has been actively involved in the design of novel antimicrobial drugs. The blueprints of these compounds were azolic…
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Heterocycles 48. Synthesis, Characterization and Biological Evaluation of Imidazo[2,1-b][1,3,4]Thiadiazole Derivatives as Anti-Inflammatory Agents
Non-steroidal anti-inflammatory drugs (NSAIDs) are an important pharmacological class of drugs used for the treatment of inflammatory diseases. They are also characterized by severe side effects, such as gastrointestinal damage, increased cardiovascular risk and renal function abnormalities. In…
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Synthesis of Novel Benzothiazole–Profen Hybrid Amides as Potential NSAID Candidates
Herein, we report the synthesis of a series of new compounds by combining 2-aminobenzothiazole with various profens. The compounds were characterized using techniques such as 1H- and 13C-NMR, FT-IR spectrometry, and high-resolution mass spectrometry (HRMS), with detailed HRMS analysis conducted for…
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Design and Synthesis of Fused Derivatives of 7-Hydroxycoumarin (Umbelliferone) with the Flavonol Quercetin and the Flavone Luteolin-Analysis of Their Antioxidant and Physicochemical Properties
Oxidative stress seems to be part of many deranged processes in the organism, affecting multiple degenerative conditions at a cellular and tissue level. Coumarins and flavonoids comprise two main categories of naturally derived compounds with multiple effects and applications. Our aim in this paper…