scholarly journals Synthesis of new pyrazolone and pyrazole-based adamantyl chalcones and antimicrobial activity

2020 ◽  
Vol 40 (9) ◽  
Author(s):  
Rawan Al-Saheb ◽  
Sami Makharza ◽  
Feras Al-battah ◽  
Rajab Abu-El-Halawa ◽  
Tawfeq Kaimari ◽  
...  
Keyword(s):  
High Dose ◽  
Moderate Activity ◽  
Dependent Manner ◽  
H Nmr ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
New Compounds ◽  
Dose Dependent ◽  
Ft Ir Spectroscopy ◽  
C Nmr

Abstract Chalcones and their derivatives are becoming increasingly popular due to their various pharmacological effects. Chalcone molecules may be extracted from natural resources, entirely synthesised, or biosynthesised by modifying the natural ones. In the present study, five pyrazole-based adamantyl heterocyclic compounds were synthesised by condensation of 1-adamantyl chalcone with substituted phenylhydrazine. The products were characterised by using ¹H NMR, ¹³C NMR and FT-IR spectroscopy. The microbiological activity of these compounds was investigated against bacteria and fungi. The new compounds showed good to moderate activity against the microbial species used for screening. All developed molecules showed antibacterial activity against Gram-negative and Gram-positive. These molecules showed antifungal activities against Fusarium oxysporum fungus and in a dose-dependent manner, apart from RS-1 molecules which showed compromised antifungal activity and even at a high dose.

Synthesis, in vitro inhibition effect of novel phthalocyanine complexes as carbonic anhydrase and paraoxonase enzyme inhibitors

2020 ◽  
Vol 24 (08) ◽  
pp. 1047-1053
Author(s):  
Emre Güzel ◽  
Barış Seçkin Arslan ◽  
Kübra Çıkrıkçı ◽  
Adem Ergün ◽  
Nahit Gençer ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Enzyme Inhibitors ◽  
Inhibition Effect ◽  
H Nmr ◽  
Vis Spectroscopy ◽  
Ft Ir ◽  
First Time ◽  
Ft Ir Spectroscopy ◽  
C Nmr

The preparation and assessment of carbonic anhydrase and paraoxonase enzyme inhibition properties of 3-(2-(5-amino-4-(4-bromophenyl)-3-methyl-1H-pyrazol-1-yl)ethoxy)phthalonitrile (2) and its nitrogen-containing non-peripheral phthalocyanine derivatives (3 and 4) are reported for the first time. The new phthalonitrile and its phthalocyanine derivatives have been elucidated by FT-IR spectroscopy, 1H-NMR, [Formula: see text]C-NMR, mass and UV-vis spectroscopy. The results demonstrated that all synthesized compounds moderately inhibited carbonic anhydrase and paraoxonase enzymes. Among the compounds, the most active ones were found to be compound 4 for PON (Ki : 0.14 [Formula: see text]M), compound 3 for hCA I (Ki : 22.52 [Formula: see text]M) and compound 1 for hCA II (Ki : 13.62 [Formula: see text]M).

scholarly journals Primary Investigation for the Mechanism of Biatractylolide fromAtractylodis Macrocephalae Rhizomaas an Acetylcholinesterase Inhibitor

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Yong-Chao Xie ◽  
Ning Ning ◽  
Li Zhu ◽  
Dan-Ning Li ◽  
Xing Feng ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Molecular Mechanisms ◽  
Acetylcholinesterase Inhibitor ◽  
Huperzine A ◽  
Dependent Manner ◽  
H Nmr ◽  
Sites Of Action ◽  
Dose Dependent ◽  
Ache Expression ◽  
C Nmr

Biatractylolide was isolated from ethyl acetate extract of driedAtractylodis Macrocephalae Rhizomaroot by multistep chromatographic processing. Structure of biatractylolide was confirmed by1H-NMR and13C-NMR. The IC50on acetylcholinesterase (AChE) activity was 6.5458 μg/mL when the control IC50value of huperzine A was 0.0192 μg/mL. Molecular Docking Software (MOE) was used to discover molecular sites of action between biatractylolide and AChE protein by regular molecular docking approaches. Moreover, biatractylolide downregulated the expression of AChE of MEF and 293T cells in a dose-dependent manner. These results demonstrated that the molecular mechanisms of inhibitory activities of biatractylolide on AChE are not only through binding to AChE, but also via reducing AChE expression by inhibiting the activity of GSK3β.

scholarly journals Synthesis of Novel Triazolo[4,3-a]Quinoxaline Darivatives Containing Pyridinyl and Thiazole Nucleous

2015 ◽  
Vol 52 ◽  
pp. 63-73
Author(s):  
Haresh G. Kathrotiya ◽  
Yogesh T. Naliapara
Keyword(s):  
Reaction Time ◽  
Elemental Analysis ◽  
High Yield ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Quinoxaline Derivatives ◽  
Ft Ir ◽  
New Compounds ◽  
C Nmr

On pursuing research about [1,2,4] triazolo [4,3-a] quinoxaline, in this paper we report a small library of novel class of [1,2,4] triazolo [4,3-a] quinoxaline derivatives containing pyridinyl thiazole moiety. Particularly valuable features of this method include high yield, broad substrate scope, shorter reaction time and straightforward procedure. The structures of new compounds have been characterized on the basis of elemental analysis, FT-IR, 1H NMR, 13C NMR, and mass spectral data.

scholarly journals A new benzothiazin-functionalized calix[4]arene-based fluorescent chemosensor for the selective and sensitive detection of Co2+ ion

2021 ◽  
Author(s):  
Fatimah Fateh ◽  
Ayşe Yildirim ◽  
Asif Ali Bhatti ◽  
Mustafa YILMAZ
Keyword(s):  
Organic Chemistry ◽  
Detection Limit ◽  
Ir Spectroscopy ◽  
Binding Constant ◽  
Spectroscopic Methods ◽  
Macrocyclic Compounds ◽  
H Nmr ◽  
Ft Ir ◽  
Ft Ir Spectroscopy ◽  
C Nmr

Abstract Calixarenes, which have a great place in supramolecular chemistry, has become the most prominent macrocyclic compounds in synthetic organic chemistry due to their easy synthesis and functionalization. In this study, p-tert-butyl calix[4]arene dihydrazide derivative was synthesized and then reacted with 3-oxo-3,4-dihydro-2H-benzo[b][1, 4] thiazin-2-ylideneacetyl chloride to prepare new calixarene based chromophore compound 4. The structure of the synthesized compound was elucidated by spectroscopic methods such as 1H-NMR 13C-NMR and FT-IR spectroscopy. Chromogenic and fluorescence properties of compound 4 were evaluated. It was observed from both studies that compound 4 was Co2+ selective and shows fluorescence Switched-off behavior. Stoichiometry, binding constant and the detection limit was calculated. The stoichiometry between compound 4 and Co2+ was found to be 1:1. The binding constant value (K) was calculated as 666.67 M− 1 using Benesi–Hildebrand equation, while the detection limit for Co2+ ion was calculated as 0.0465 µM.

scholarly journals Homogeneous Esterification of Cellulose in the Mixture N-Butylpyridinium Chloride/Dimethylsulfoxide

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Lahcen El Hamdaoui ◽  
Mohammed El Moussaouiti ◽  
Said Gmouh
Keyword(s):  
Reaction Medium ◽  
Reaction Parameters ◽  
Reaction Conditions ◽  
Cellulose Esters ◽  
Short Reaction Time ◽  
H Nmr ◽  
Mild Conditions ◽  
Ft Ir ◽  
Ft Ir Spectroscopy ◽  
C Nmr

The present study deals with the homogeneous acylation of cellulose withp-nitrobenzoyl chloride in a reaction medium composed of a mixture of 1-butylpyridinium chloride and dimethylsulfoxide (BPyCl/DMSO), in the presence of different bases and under mild conditions. The preparation of cellulosep-nitrobenzoate depending on the reaction conditions, the influences of reaction parameters such as the base type, and the types of cellulose (kraft and microcrystalline) on the products were investigated. Cellulosep-nitrobenzoate with a degree of substitution (DS) in the range from 0.12 to 1.5 was accessible, with a low excess of reagent and for a short reaction time. The cellulose esters were characterized by1H-NMR,13C NMR, and FT-IR spectroscopy, thermogravimetric analysis (TGA), scanning electron microscopy (SEM), and solubility tests.

scholarly journals Synthesis and Biological Evaluation of Novel Piperazine Containing Hydrazone Derivatives

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Betül Kaya ◽  
Yusuf Özkay ◽  
Halide Edip Temel ◽  
Zafer Asım Kaplancıklı
Keyword(s):  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Standard Drug ◽  
H Nmr ◽  
Chemical Structures ◽  
Ft Ir ◽  
Inhibition Potency ◽  
New Compounds ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

Some hydrazone derivatives were synthesized and their potential anticholinesterase activities were examined. A series of eleven new compounds of N′-(2,4-disubstitutedbenzylidene)-2-(4-(4-nitrophenyl)piperazin-1-yl)acetohydrazide derivatives were obtained via reaction of 2-[4-(4-nitrophenyl)piperazin-1-yl]acetohydrazide with aromatic aldehydes. The chemical structures of the compounds were enlightened by FT-IR,1H-NMR,13C-NMR, and HRMS (ESI) spectral data. The inhibition potency of the compounds3a–kagainst AChE and BuChE was measured and evaluated using a modification of Ellman’s spectrophotometric method. Among the tested compounds, compound3cwas assigned to be the most active derivative. Galantamine was used as a standard drug.

scholarly journals Synthesis of triarylpyridines with sulfonate and sulfonamide moieties via a cooperative vinylogous anomeric-based oxidation

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Morteza Torabi ◽  
Mohammad Ali Zolfigol ◽  
Meysam Yarie ◽  
Behrouz Notash ◽  
Saeid Azizian ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Current Trend ◽  
X Ray ◽  
H Nmr ◽  
Catalytic Application ◽  
Transmission Electron ◽  
Ft Ir ◽  
Derivative Thermogravimetry ◽  
Ft Ir Spectroscopy ◽  
C Nmr

AbstractHerein, novel magnetic nanoparticles with pyridinium bridges namely Fe3O4@SiO2@PCLH-TFA through a multi-step pathway were designed and synthesized. The desired catalyst and its corresponding precursors were characterized with different techniques such as Fourier transform infrared (FT-IR) spectroscopy, 1H NMR, 13C NMR, Mass spectroscopy, energy dispersive X-ray (EDX) analysis, thermogravimetric/derivative thermogravimetry (TG/DTG) analysis, scanning electron microscopy (SEM), transmission electron microscopy (TEM), and vibrating sample magnetometer (VSM). In addition, the catalytic application of the prepared catalyst in the synthesis of new series of triarylpyridines bearing sulfonate and sulfonamide moieties via a cooperative vinylogous anomeric-based oxidation was highlighted. The current trend revealed that the mentioned catalyst shows high recoverability in the reported synthesis.

scholarly journals High-dose Glycerol Monolaurate Up-Regulated Beneficial Indigenous Microbiota without Inducing Metabolic Dysfunction and Systemic Inflammation: New Insights into Its Antimicrobial Potential

Nutrients ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 1981 ◽  
Author(s):  
Qiufen Mo ◽  
Aikun Fu ◽  
Lingli Deng ◽  
Minjie Zhao ◽  
Yang Li ◽  
...  
Keyword(s):  
Lipid Metabolism ◽  
Systemic Inflammation ◽  
Body Weight Gain ◽  
High Dose ◽  
Dependent Manner ◽  
Glucose And Lipid Metabolism ◽  
Glycerol Monolaurate ◽  
Indigenous Microbiota ◽  
Anti Inflammatory ◽  
Dose Dependent

Glycerol monolaurate (GML) has potent antimicrobial and anti-inflammatory activities. The present study aimed to assess the dose-dependent antimicrobial-effects of GML on the gut microbiota, glucose and lipid metabolism and inflammatory response in C57BL/6 mice. Mice were fed on diets supplemented with GML at dose of 400, 800 and 1600 mg kg−1 for 4 months, respectively. Results showed that supplementation of GML, regardless of the dosages, induced modest body weight gain without affecting epididymal/brown fat pad, lipid profiles and glycemic markers. A high dose of GML (1600 mg kg−1) showed positive impacts on the anti-inflammatory TGF-β1 and IL-22. GML modulated the indigenous microbiota in a dose-dependent manner. It was found that 400 and 800 mg kg−1 GML improved the richness of Barnesiella, whereas a high dosage of GML (1600 mg kg−1) significantly increased the relative abundances of Clostridium XIVa, Oscillibacter and Parasutterella. The present work indicated that GML could upregulate the favorable microbial taxa without inducing systemic inflammation and dysfunction of glucose and lipid metabolism.

Ultrasound-assisted aqua-mediated synthesis of multi-substituted tetrahydropyridine-3-carboxylates using N-carboxymethyl-3-pyridinium hydrogensulfate ([N-CH2CO2H-3-pic]+HSO4−) as a new efficient ionic liquid catalyst

2021 ◽  
Vol 3 (6) ◽  
Author(s):  
Kobra Nikoofar ◽  
Fatemeh Shahriyari
Keyword(s):  
Ionic Liquid ◽  
Reaction Times ◽  
Aromatic Aldehydes ◽  
Environmentally Benign ◽  
H Nmr ◽  
Sonic Waves ◽  
Ft Ir ◽  
High Yields ◽  
Work Up ◽  
C Nmr

AbstractA simple, straightforward, and ultrasound-promoted method for the preparation of some highly functionalized tetrahydropyridines reported via pseudo five-component reaction of (hetero)aromatic aldehydes, different anilines, and alkyl acetoacetates in the presence of [N-CH2CO2H-3-pic]+HSO4−, as a novel ionic liquid, in green aqueous medium. The IL was synthesized utilizing simple and easily-handled substrates and characterized by FT-IR, 1H NMR, 13C NMR, GC-MASS, FESEM, EDX, and TGA/DTG techniques. The procedure contains some highlighted aspects which are: (a) performing the MCR in the presence of aqua and sonic waves, as two main important and environmentally benign indexes in green and economic chemistry, (b) high yields of products within short reaction times, (c) convenient work-up procedure, (d) preparing the new IL via simple substrates and procedure.

scholarly journals Effect of Synchronous Versus Sequential Regimens on the Pharmacokinetics and Biodistribution of Regorafenib with Irradiation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 386
Author(s):  
Tung-Hu Tsai ◽  
Yu-Jen Chen ◽  
Li-Ying Wang ◽  
Chen-Hsi Hsieh
Keyword(s):  
Stereotactic Body Radiation Therapy ◽  
In Vivo Studies ◽  
Control Group ◽  
High Dose ◽  
Dependent Manner ◽  
Hep G2 ◽  
Time Curve ◽  
Dose Dependent

This study was performed to evaluate the interaction between conventional or high-dose radiotherapy (RT) and the pharmacokinetics (PK) of regorafenib in concurrent or sequential regimens for the treatment of hepatocellular carcinoma. Concurrent and sequential in vitro and in vivo studies of irradiation and regorafenib were designed. The interactions of RT and regorafenib in vitro were examined in the human hepatoma Huh-7, HA22T and Hep G2 cell lines. The RT–PK phenomenon and biodistribution of regorafenib under RT were confirmed in a free-moving rat model. Regorafenib inhibited the viability of Huh-7 cells in a dose-dependent manner. Apoptosis in Huh-7 cells was enhanced by RT followed by regorafenib treatment. In the concurrent regimen, RT decreased the area under the concentration versus time curve (AUC)regorafenib by 74% (p = 0.001) in the RT2 Gy × 3 fraction (f’x) group and by 69% (p = 0.001) in the RT9 Gy × 3 f’x group. The AUCregorafenib was increased by 182.8% (p = 0.011) in the sequential RT2Gy × 1 f’x group and by 213.2% (p = 0.016) in the sequential RT9Gy × 1 f’x group. Both concurrent regimens, RT2Gy × 3 f’x and RT9Gy × 3 f’x, clearly decreased the biodistribution of regorafenib in the heart, liver, lung, spleen and kidneys, compared to the control (regorafenib × 3 d) group. The concurrent regimens, both RT2Gy × 3 f’x and RT9Gy × 3 f’x, significantly decreased the biodistribution of regorafenib, compared with the control group. The PK of regorafenib can be modulated both by off-target irradiation and stereotactic body radiation therapy (SBRT).

Sign in / Sign up

Export Citation Format

Share Document