scholarly journals Synthesis of 1,2,3-triazole derivatives based on propargyl ester of a saturated single-basic carbonic acid and para-azidobenzoic acid

2021 ◽  
Vol 12 (1) ◽  
pp. 13-17
Author(s):  
Ibragimdjan Аbdugafurov Azizovich ◽  
Fazliddin Qirgizov Bakhtiyarovich ◽  
Ilhom Оrtikov Sobirovich
Keyword(s):  
Carbonic Acid ◽  
Effect Of Temperature ◽  
Reaction Yield ◽  
Factors Affecting ◽  
Low Toxicity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
First Time ◽  
Derivatives Of ◽  
Membered Heterocycle

The development of highly effective and low-toxicity nonsteroidal anti-inflammatory drugs (NSAIDs) is one of the important challenges facing modern pharmacology. To overcome this problem, many studies have been conducted on compounds containing a five-membered heterocycle containing three nitrogen atoms. The pharmacodynamics of these compounds are mainly due to their anti-inflammatory effect. Therefore, it is important to synthesize new derivatives of 1,2,3-triazoles, to determine their structure and to look for substances with anti-inflammatory activity on their basis. For the first time, the corresponding derivatives of 4-(4-(exchangeable)-1H-1,2,3-triazole-1-yl)-benzoic acid were synthesized by cycloaddition of propargyl esters of saturated carboxylic acids and para-azidobenzoic acid in the presence of copper (I) iodide. The structure of the obtained substances was analyzed by IR, 1H NMR, and MS techniques. It is proved that under the action of the catalyst in the reaction, only 1,4-isomers are formed. Factors affecting the course of the reaction were identified. Only one isomer is formed in the reaction of cyclic addition under the action of a catalyst and the effect of temperature, duration of time, and nature of the solvent on the reaction yield was studied.

Cytostatic and Antiviral Activity Evaluations of Hydroxamic Derivatives of Some Non-steroidal Anti-inflammatory Drugs

2009 ◽  
Vol 73 (3) ◽  
pp. 328-338 ◽  
Author(s):  
Zrinka Rajic ◽  
Ivan Butula ◽  
Branka Zorc ◽  
Sandra Kraljevic Pavelic ◽  
Karlo Hock ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Derivatives Of

scholarly journals Active Anti-Inflammatory and Hypolipidemic Derivatives of Lorazepam

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3277
Author(s):  
Panagiotis Theodosis-Nobelos ◽  
Georgios Papagiouvannis ◽  
Panos N. Kourounakis ◽  
Eleni A. Rekka
Keyword(s):  
Acute Inflammation ◽  
Current Knowledge ◽  
Rat Plasma ◽  
Straightforward Method ◽  
Inflammatory Drugs ◽  
Multifunctional Agents ◽  
Anti Inflammatory ◽  
High Yields ◽  
Derivatives Of ◽  
And Oxidative Stress

Novel derivatives of some non steroidal anti-inflammatory drugs, as well as of the antioxidants α-lipoic acid, trolox and (E)-3-(3,5-di-tert-butyl-4-hydroxyphenyl)acrylic acid with lorazepam were synthesised by a straightforward method at satisfactory to high yields (40%–93%). All the tested derivatives strongly decreased lipidemic indices in rat plasma after Triton induced hyperlipidaemia. They also reduced acute inflammation and a number of them demonstrated lipoxygenase inhibitory activity. Those compounds acquiring antioxidant moiety were inhibitors of lipid peroxidation and radical scavengers. Therefore, the synthesised compounds may add to the current knowledge about multifunctional agents acting against various disorders implicating inflammation, dyslipidaemia and oxidative stress.

Synthesis and pharmacological evaluation of amide derivatives of non-steroidal anti-inflammatory drugs

1992 ◽  
Vol 1 (3) ◽  
pp. 201-212 ◽  
Author(s):  
M. -F. Otis ◽  
L. Levesque ◽  
F. Marceau ◽  
J. Lacroix ◽  
R. C. Gaudreault
Keyword(s):  
Pharmacological Evaluation ◽  
Amide Derivatives ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Derivatives Of

scholarly journals Nutraceutical Properties of Mulberries Grown in Southern Italy (Apulia)

Antioxidants ◽  
2019 ◽  
Vol 8 (7) ◽  
pp. 223 ◽  
Author(s):  
Carmine Negro ◽  
Alessio Aprile ◽  
Luigi De Bellis ◽  
Antonio Miceli
Keyword(s):  
High Performance ◽  
Southern Italy ◽  
Morus Alba ◽  
Array Detector ◽  
Morus Nigra ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Mulberry Fruits ◽  
First Time ◽  
Gallic Acid Equivalent

In this work, for the first time, were analyzed mulberry genotypes grown in Apulia (Southern Italy, Salento region) were analyzed. Two local varieties of Morus alba (cv. Legittimo nero and cv. Nello) and one of Morus nigra were characterized for content in simple sugars, organic acids, phenols, anthocyanins; fruit antioxidant activity (AA) was also evaluated by three different methods (2,2-Diphenyl-1-picrylhydrazyl, DPPH; 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), ABTS; and Ferric reducing antioxidant potential, FRAP test). The results showed that the sugars amount ranged between 6.29 and 7.66 g/100 g fresh weight (FW) while the malic and citric acids content was low, at about 0.1–1 g/100 g FW. Mulberries are a good source of phenols which are present in higher values in M. nigra and M. alba cv. Legittimo nero (485 and 424 mg Gallic Acid Equivalent (GAE)/ 100 g FW, respectively). The high performance liquid chromatography/diode array detector/mass spectrometry (HPLC/DAD/MS) analysis identified 5 main anthocyanin compounds present in different concentrations in each variety of mulberry: cyanidin 3-sophoroside, cyanidin 3-glucoside, cyanidin 3-rutinoside, pelargonidin 3-glucoside, pelargonidin 3-rutinoside. The highest concentration of anthocyanins was determined in Morus alba Legittimo (about 300 mg/100 g FW) while the lowest content (about 25 mg/100 g FW) was measured in M. alba cv. Nello. Morus nigra showed a good AA in comparison with the different M. alba genotypes with all the used methods; its AA was equal to 33, 26 and 21 μmols Trolox/g FW when using DPPH, ABTS and FRAP tests, respectively. All genotypes showed an anti-inflammatory activity (measured by cyclooxygenase (COX) inhibitory assay) which was also compared with two commercial anti-inflammatory drugs. The data obtained support the high biological qualities of mulberry fruits and their diffusion in human nutrition.

scholarly journals Nitroxide derivatives of non-steroidal anti-inflammatory drugs exert anti-inflammatory and superoxide dismutase scavenging properties in A459 cells

2012 ◽  
Vol 165 (4b) ◽  
pp. 1058-1067 ◽  
Author(s):  
Wilmarie Flores-Santana ◽  
Terry Moody ◽  
Weibin Chen ◽  
Michael J Gorczynski ◽  
Mai E Shoman ◽  
...  
Keyword(s):  
Superoxide Dismutase ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Derivatives Of

scholarly journals Modulating the Chemical and Biological Properties of Cancer Stem Cell-Potent Copper(II)-Nonsteroidal Anti-Inflammatory Drug Complexes

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1677 ◽  
Author(s):  
Shin ◽  
Eskandari ◽  
Suntharalingam
Keyword(s):  
Three Dimensional ◽  
Biological Properties ◽  
Culture Studies ◽  
Apoptosis Pathway ◽  
Cytotoxicity Studies ◽  
Ic50 Value ◽  
Low Toxicity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Micromolar Range

Copper(II) complexes bearing nonsteroidal anti-inflammatory drugs (NSAIDs) are known to potently kill cancer stem cells (CSCs), a subpopulation of tumour cells with high metastatic and relapse fidelity. One of the major disadvantages associated to these copper(II) complexes is their instability in the presence of strong cellular reductants (such as ascorbic acid). Here we present a biologically stable copper(II)-NSAID complex containing a bathocuproinedisulfonic acid disodium ligand and two indomethacin moieties, Cu(bathocuproinedisulfonic acid disodium)(indomethacin)2, 2. The copper(II) complex, 2 kills bulk breast cancer cells and breast CSC equally (in the sub-micromolar range) and displays very low toxicity against non-tumorigenic breast and kidney cells (IC50 value > 100 µM). Three-dimensional cell culture studies show that 2 can significantly reduce the number and size of breast CSC mammospheres formed (from single suspensions) to a similar level as salinomycin (an established anti-breast CSC agent). The copper(II) complex, 2 is taken up reasonably by breast CSCs and localises largely in the cytoplasm (>90%). Cytotoxicity studies in the presence of specific inhibitors suggest that 2 induces CSC death via a reactive oxygen species (ROS) and cyclooxygenase isoenzyme-2 (COX-2) dependent apoptosis pathway.

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