scholarly journals Design, Synthesis, andIn VitroAntioxidant Activity of 1,3,5-Trisubstituted-2-pyrazolines Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
P. C. Jagadish ◽  
Neeraj Soni ◽  
Amita Verma

Mannich base of pyrazolines 3(a–e) under both conventional and microwave irradiation was synthesized. All the synthesised compounds were purified by recrystallisation, characterized on the basis of UV, IR, and NMR spectroscopy, and further supported by mass spectroscopy. The result obtained confirms superiority of microwave irradiation method over classical heating one. The molecular properties and Lipinski rule of five for compounds 3(a–e) were determined by Molinspiration. The synthesized compounds were subsequently evaluated for the antioxidant activity. All the compounds were found in compliance with Lipinski “Rule of Five”, and compound 3e havingp-hydroxyl substitution showed best antioxidant activity as compared to ascorbic acid and rutin.

1988 ◽  
Vol 43 (2) ◽  
pp. 165-170 ◽  
Author(s):  
Whei Oh Lin ◽  
Maria C. B. V. de Souza ◽  
Helmut G. Alt

The synthesis of trans-1.2-cyclohexanedioxydiacetamides starting with trans-1.2-cyclohexane-diol is described. Eleven of these compounds are characterized by IR, 1H NMR, 13C NMR and mass spectroscopy as well as elemental analyses. Most of these compounds are suitable ionophors for the cations K+ and Ca2+. The coordination sites of these ligands in the 1:2 complexes were determined by IR and NMR spectroscopy


Author(s):  
Rania B. Bakr ◽  
Nadia A.A. Elkanzi

Background & objectives: 1,2-thiazine and pyridine heterocycles drew much attention due to their biological activities including antioxidant activity. Based upon fragment based drug design, novel pyrido[1,2]thiazines 9a-c, thiazolidinopyrido[1,2]thiazines 10a-c and azetidinopyrido[1,2]thiazines 11a-c were designed and prepared. Methods: These novel derivatives 9a-c, 10a-c and 11a-c were subjected to screening for their antioxidant activity via various assays as DPPH radical scavenging potential, reducing power assay and metal chelating potential. Results: All the assayed derivatives exhibited excellent antioxidant potential and the tested compounds 9a, 9b, 10a, 10b, 11a and 11b exhibited higher DPPH scavenging potential (EC50 = 32.7, 53, 36.1, 60, 40.6 and 67 µM, respectively) than ascorbic acid (EC50 = 86.58 µM). While targets 9a, 10a and 11a (RP50 = 52.19, 59.16 and 52.25 µM, respectively) exhibited better reducing power than the ascorbic acid (RP50 = 84.66 µM). Computational analysis had been utilized to prophesy the bioactivity and molecular properties of the target compounds. Conclusion: To predict the binding manner of the novel derivatives as antioxidants, in-silico docking study had been performed to all the newly prepared compounds inside superoxide dismutase (SOD) and catalase (CAT) active site. The most active antioxidant candidate 9a (EC50 = 32.7 µM, RP50 = 52.19 µM) displayed excellent binding with Lys134 amino acid residing at Cu-Zn loop of SOD with binding energy score = -7.54 Kcal/mol thereby increase SOD activity and decrease reactive oxygen species.


2019 ◽  
Vol 10 (2) ◽  
pp. 1510-1515
Author(s):  
Taiseer Abdul-Kader Saleh ◽  
Rafah Razooq Hameed Al-Samarrai ◽  
Noor Essam Abdul-Razzaq

This study was carried out to synthesise some new Schiff bases compounds through condensation of ascorbic acid (keto form) with some compounds which have amine group in their structure also these compounds synthesized by using of microwave irradiation and traditional method and compare the results obtained. Microwave irradiation of organic reactions has quickly acquired popularity as it increases the speed of the reaction towards multiple kinds of synthetic transformations, solventless procedures without the use of supporting reagents and therefore eco-friendly, the antioxidant properties were studied for all compounds included in this study, the results indicate that IC50 for the compounds synthesized by using of microwave irradiation method were higher than the traditional method, and also the biological activity of the prepared compounds were also studied to estimate capability of suppressing Enterococcus, Staphyllo coccus aureus and E. Coli than the starting materials that have biological activity on these bacteria. This study shows that the diameters of inhibitions in Petri dishes have higher and wider at a concentration (10 mg / ml) for used bacteria.


2006 ◽  
Vol 61 (11) ◽  
pp. 1421-1425 ◽  
Author(s):  
Maasoomeh Tabatabaee ◽  
Mitra Ghassemzadeh ◽  
Behnaz Zarabi ◽  
Bernhard Neumüllerc

Reaction of 4-amino-6-methyl-3-thio-3,4-dihydro-1,2,4-triazin-5(2H)-one (1) with 2-methoxybenzaldehyde, 4-methoxybenzaldehyde, 2-pyridinecarbaldehyde, and 2,4-dichlorobenzaldehyde under classical heating and microwave irradiation in a solventfree system led to the corresponding imines (Schiff bases) 2-5. All synthesized compounds have been characterized by IR and NMR spectroscopy, mass spectrometry and by X-ray diffraction studies.


2011 ◽  
Vol 6 (12) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Joyce J. Kiplimo ◽  
Md. Shahidul Islam ◽  
Neil A. Koorbanally

The dichloromethane extract of the aerial part of the plant Vepris glomerata (Rutaceae) yielded a new flavonoid, which was accorded the trivial name veprisinol (1), together with four known furoquinoline alkaloids: haplopine-3,3′-dimethylallyl ether (2), anhydroevoxine (3), evoxine (4) and skimmianine (5). The structures of the compounds were established by 1D and 2D NMR spectroscopy, as well as HREIMS. Compounds 1 and 2 have strong antioxidant potential, similar to and in some instances better than ascorbic acid and can be used as beneficial additives to antioxidant supplements.


2017 ◽  
Vol 68 (3) ◽  
pp. 474-477
Author(s):  
Lacramioara Oprica ◽  
Doina Atofanei ◽  
Vladimir Poroch

The amounts of anthocyanins, flavonoids, total polyphenol and ascorbic acid in seven apple cultivars from Romania were investigated. The amounts of polyphenol and flavonoids in pulp and skin of apple cultivars ranged between 17.18�7.52 mg GAE/g DW and 20.10�11.06 mg CE/g DW as well as 3.64�1.18 mg GAE/g DW and 10.31�5.57 mg CE/g DW, respectively. The highest and smallest values of ascorbic acid both in the skin and the pulp were observed in the cultivars Mutsu and Starkrimson. The anthocyanin content is positively correlated with the colour intensity of the apple epicarp, being about three-fold higher in Prima than Golden Delicious cultivar. The better antioxidant activity provided by the content of polyphenol, ascorbic acid and flavonoids was in apple fruits of Mutsu cultivar and for this reason it should be regarded as a valuable source of antioxidants.


2008 ◽  
Vol 59 (1) ◽  
pp. 41-44
Author(s):  
Maria-Daniela Sofei ◽  
Maria Ilici ◽  
Valentin Badea ◽  
Carol Csunderlik ◽  
Vasile-Nicolae Bercean

The synthesis of 1H-3-aryl-7-ethoxycarbonyl-6-methyl-pyrazolo[5,1-c][1,2,4]triazoles (2) was carried out by cyclization of 1H-5-arylidenehydrazino-4-ethoxycarbonyl-3-methyl-pyrazoles (1) in the presence of bromine using glacial acetic acid as solvent and sodium acetate as base. The new nine obtained compounds were characterized by IR and NMR spectroscopy and mass spectrometry.


2018 ◽  
Vol 69 (5) ◽  
pp. 1041-1044
Author(s):  
Claudia Anca Mot ◽  
Andreea I. Lupitu ◽  
Simona Bungau ◽  
Ciprian Iovan ◽  
Dana Maria Copolovici ◽  
...  

The aim of this study was to determine the phenolic content and antioxidant activity of extracts obtained from herb of Tanacetum vulgare L. (tansy) harvested in two different locations from the western part of Romania. Aqueous extracts of tansy presented high antioxidant activity that ranged between 295.77 and 653.65 mg GAE/L, and remarkable percentage of inhibition (31.82-65.05 %). The compounds quantified in the plant extracts that were determined by UHPLC are: ascorbic acid, riboflavin, pyrocatechol, rutin, quercetin, and kaempferol. Extracts obtained from tansy flowers showed higher content of phenols compared to that obtained from leaves. Similarly, the flower extracts present a high antioxidant activity that could suggest their use as natural additives in food preservation and also in pharmaceutical industry and veterinary medicine.


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