scholarly journals 2-{[(4-Hydroxy-3,5-dimethoxyphenyl)methylidene]hydrazinylidene}-4-oxo-1,3-thiazolidin-5-yl Acetic Acid

Molbank ◽  
10.3390/m1009 ◽  
2018 ◽  
Vol 2018 (3) ◽  
pp. M1009 ◽  
Author(s):  
Sangeetha Karanth ◽  
Badiadka Narayana ◽  
Sharath Kodandoor ◽  
Balladka Sarojini
Keyword(s):  
Acetic Acid ◽  
Title Compound ◽  
Radical Scavenging ◽  
Antioxidant Property ◽  
Mass Spectral ◽  
Bacterial Enzyme ◽  
Ft Ir ◽  
Antibacterial And Antifungal

Thia-Michael addition of 2-[(4-hydroxy-3,5-dimethoxyphenyl)methylidene]hydrazine-1-carbothioamide (1) with maleic anhydride results in the formation of the title compound 2-{[(4-hydroxy-3,5-dimethoxyphenyl)methylidene]hydrazinylidene}-4-oxo-1,3-thiazolidin-5-yl acetic acid 2. The precursor 1 is synthesized by the reaction of 4-hydroxy-3,5-dimethoxybenzaldehyde and thiosemicarbazide in the presence of glacial acetic acid as the catalyst. The structure of the title compound is determined by elemental analysis, FT-IR, 1H-NMR, 13C-NMR and mass spectral data. In order to determine the molecular interactions with the bacterial enzyme, the title compound is further docked into the active site of the MurB protein of Staphylococcus aureus (PDB ID: 1HSK). The in vitro antibacterial and antifungal activity of the title compound is carried out in order to appraise its antimicrobial efficacy by determination of zone of inhibition and minimal inhibitory concentration. The compound is also evaluated for its antioxidant property by 2,2-diphenyl-1-picryl-hydrazyl (DPPH) radical scavenging assay.

scholarly journals Synthesis, Characterization and Molecular Docking of 1,2,4-Triazole Derivatives as Potential Antimicrobial Agents

2020 ◽  
Vol 32 (6) ◽  
pp. 1437-1442
Author(s):  
Panneerselvam Kalaivani ◽  
Jayaraman Arikrishnan ◽  
Mannuthusamy Gopalakrishnan
Keyword(s):  
Antimicrobial Agents ◽  
Docking Study ◽  
Binding Mode ◽  
Zone Of Inhibition ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Inhibition Concentration ◽  
Ft Ir ◽  
Antibacterial And Antifungal

In this study, a new series of (E)-N-(4-(3-(3,5-dialkylphenyl)acryloyl)phenyl)-2-(1H-1,2,4-triazol-1- yl)acetamide (32-41) was synthesized, characterized by FT-IR, 1H NMR, 13C NMR and Mass spectral analysis and evaluated for their in vitro antibacterial and antifungal activities. The docking study of the newly synthesized compounds was performed and results showed good binding mode in the active site of 1T9U protein. The zone of inhibition concentration was tested for the synthesized compounds against five bacterial and three fungal strains. Compounds 34 and 37 have good antibacterial activity. Compounds 3, 4 and 6 shows moderate inhibition against the antifungal activity.

scholarly journals Flavonoids inJuglans regiaL. Leaves and Evaluation ofIn VitroAntioxidant Activity via Intracellular and Chemical Methods

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Ming-Hui Zhao ◽  
Zi-Tao Jiang ◽  
Tao Liu ◽  
Rong Li
Keyword(s):  
High Performance ◽  
Juglans Regia ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Dry Weight ◽  
Negative Ion ◽  
Chemical Methods ◽  
Mass Spectral

Flavonoids are rich inJuglans regiaL. leaves. They have potent antioxidant properties, which have been related to regulating immune function and enhancing anticancer activity. Herein, qualitative and quantitative determination of flavonoids fromJ. regialeaves was carried out using high performance liquid chromatography coupled with tandem mass spectrometry with electrospray ionization and negative ion detection (HPLC-ESI-MS/MS) by comparison of the retention times and mass spectral fragments with standard substances or related literatures. Seventeen compounds were identified and major components are quercetin-3-O-rhamnoside (453.11 μg/g, dry weight), quercetin-3-O-arabinoside (73.91 μg/g), quercetin-3-O-xyloside (70.04 μg/g), kaempferol-O-pentoside derivative (49.04 μg/g), quercetin-3-O-galactoside (48.61 μg/g), and kaempferol-O-pentoside (48.46 μg/g). Thein vitrointracellular antioxidation indicated that flavonoids fromJ. regialeaves could reduce the reactive oxygen species (ROS) level in RAW264.7 cells and showed good radical scavenging activities. These results proved to be more related to the flavonoids that could be considered in the design of new formulations of dietary supplements or functional foods.

scholarly journals Synthesis, structural characterization and antimicrobial evaluation of some novel piperidin-4-one oxime esters

2015 ◽  
Vol 80 (9) ◽  
pp. 1101-1111 ◽  
Author(s):  
Gokula Krishnan ◽  
R. Sivakumar ◽  
V. Thanikachalam
Keyword(s):  
Biologically Active ◽  
Good Activity ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Xrd Study ◽  
Antimicrobial Evaluation ◽  
Ft Ir ◽  
Antibacterial And Antifungal

Fifteen novel biologically active piperidin-4-one oxime esters (8-22) have been synthesized with good yields. These compounds were prepared from in-situ activated carboxylic acids using POCl3 and pyridine with piperidin-4- one oximes. The structure of the title compounds were elucidated on the basis of FT-IR, NMR (1D and 2D) and mass spectral analyses. The single crystal XRD study of compounds 12 and 20 were the further evidence for the proposed structure unambiguously. All the synthesized compounds were tested for in vitro antibacterial and antifungal activities. Many of these derivatives exhibited good activity against Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, Trigoderma veride and Aspergillus flavus.

scholarly journals Phytochemical evaluation and antioxidant assay of ethanolic extracts of traditional medicinal plants (Ferula assafoetida, Saussurea costus, Peganum harmala) in oman

2017 ◽  
Vol 9 (1) ◽  
pp. 132 ◽  
Author(s):  
S Hemadri Reddy ◽  
Aysha Al-Weheib ◽  
Halima Al Shekaili ◽  
Rehab Al-Naabi
Keyword(s):  
Radical Scavenging ◽  
Natural Antioxidants ◽  
Antioxidant Property ◽  
Total Phenolic ◽  
Peganum Harmala ◽  
Phytochemical Investigation ◽  
Ferula Assafoetida ◽  
Phenolic And Flavonoid

<p><em>Ferula assafoetida, Saussurea costus</em> and  <em>Peganum harmala</em> are considered an important traditional folk medicines in Oman, extracts of these plants were screened for assessing bioactive phytochemical constituents and their antioxidant property. Total phenolic and flavonoid contents were evaluated to explore the reliable and potential sources of novel natural antioxidants. Preliminary phytochemical screening of different plant extracts and phytochemical investigation showed variations in the presence and amount of active ingredients. All the fractions of <em>P.harmala</em>, <em>S.costus and F.assafoetida have </em>flavonoid and phenolic compounds, whereas, the highest amount was found in <em>F.assafoetida which was </em>0.370, 0.053 mg/ml respectively. Under antioxidant study the H<sub>2</sub>O<sub>2</sub> free radical scavenging potential and Phosphomolybdate assay were studied <em>in vitro</em> for the determination of antioxidant activity. However <em>S. costus</em> extract showed the highest scavenging percentages 89%. In Phosphomolybdate assay <em>Ferula assafoetida </em>has a very good antioxidant potential due to   phenolic and flavonoid components.</p>

Phytochemical and Pharmacological Activity of Myristica fragrans Houtt (Myristicaceae)

2017 ◽  
Vol 9 (01) ◽  
Author(s):  
Md Arifur Rahman Chowdhury ◽  
Manirujjaman . ◽  
Md Mazedul Haq
Keyword(s):  
Acetic Acid ◽  
Phenolic Content ◽  
Methanolic Extract ◽  
Radical Scavenging ◽  
Antioxidant Property ◽  
Free Radical Scavenging ◽  
Total Phenolic ◽  
Writhing Test ◽  
Myristica Fragrans ◽  
Myristica Fragrans Houtt

Objective: Myristica fragrans Houtt commonly used as traditional medicine for alleviating of various disorders. The purpose of our study was to map out the in vitro antioxidant property and in vivo anti-hyperglycemic and analgesic effect of the methanolic extract of Myristica fragrans Houtt. (Seed and mace) (Myristicaceae) on Swiss albino mice. Methods: The processed powder of Myristica fragrans Houtt (seed and mace) were subjected to methanolic extraction by soxhlet filtration methods, and the desiccated extract was used for screening of antioxidant by DPPH free radical scavenging assessment as well as total phenolic content by using folin-ciocalteu reagent.Anti-hyperglycemic effect and analgesic action tested through alloxan induced antidiabetics test and acetic acid-tempted writhing test on mice. Results: In DPPH free radical scavenging assessment, free radicals neutralization expressed as % of inhibition 49.69±0.06% also by IC50 values as 68.43 µg/ml surmise middle level of antioxidant property. The total phenolic content expressed as 186.25 mg/g equivalent of gallic acid indicates, active phenolic content. Oral administration of 200 and 400 mg/kg of extract dose and reference drug vildagliptin (50 mg/kg) for the duration of the 4-day study period, and initiated % of inhibition the blood glucose level measured as 22.48%, 44.78% and 62.02% regard as the significant anti-hyperglycemic properties. The analgesic activity was investigated by using the acetic acid-induced writhing test in mice, at the dose of 200 mg/kg body and 400mg/kg weight, and resulting 50.4% and 68.10% correspondingly, which was considerably significant with a standard drug. Conclusion: The present study suggests that methanolic extract of seed and mace of Myristica fragrans Houtt can manage moderate oxidative stress as well as perform the painkilling action. Besides, prolong medication may enhance the new dimension of anti-hyperglycemic activity.

Extraction, Chemical Composition, Antioxidant Property and In vitro Anticancer Activity of Silymarin from Silybum Marianum On Kb and A549 Cell Lines

2020 ◽  
Vol 17 ◽  
Author(s):  
Mojgan Azadpour ◽  
Mohammad Mehdi Farajollahi ◽  
Ali Mohammad Varzi ◽  
Pejman Hashemzadeh ◽  
Hossein Mahmoudvand ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
A549 Cell ◽  
Hplc Analysis ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antioxidant Property ◽  
Silybum Marianum ◽  
Stable Free Radical

Introduction: This study aimed to evaluate the antioxidant property of silymarin (SM) extracted from the seed of Silybum marianum and its anticancer activity on KB and A549 cell lines following 24, 48, and 72 h of treatment. Methods: Ten grams of powdered S. marianum seeds were defatted using n-hexane for 6 hours and then extracted by methanol. The silymarin extracted of extraction components The extracted components of silymarin were measured by spectrophotometric assay and HPLC analysis. 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, phenol content, total flavonoid content, and total antioxidant capacity were measured to detect the antioxidant properties of SM. The anticancer activity of the SM on cell lines evaluated by MTT. Results: In HPLC analysis, more than 50% of the peaks were related to silibin A and B. SM was reducedDPPH (the stable free radical) with a 50% inhibitory concentration (IC50) of 6.56 μg/ ml in comparison with butylated hydroxyl toluene (BHT), which indicated an IC50 of ~3.9 μg/ ml.The cytotoxicity effect of SM on the cell lines was studied by MTT assay. The cytotoxicity effect of the extracted silymarin on KB and A549 cell lines was observed up to 80 and 70% at 156 and 78 µg/ml, respectively. The IC50 value of the extracted SM on KB and A549 cell lines after 24 hours of treatment was seen at 555 and 511 µg/ml, respectively. Conclusion: Due to the good antioxidant and anticancer properties of the isolated silymarin, its use as an anticancer drug is suggested.

Synthesis, SAR, In-Silico appraisal and Anti-Microbial Study of substituted 2-aminobenzothiazoles derivatives

2019 ◽  
Vol 15 ◽  
Author(s):  
Devidas G. Anuse ◽  
Suraj N. Mali ◽  
Bapu R. Thorat ◽  
Ramesh S. Yamgar ◽  
Hemchandra K. Chaudhari
Keyword(s):  
Antimicrobial Activity ◽  
In Silico ◽  
Docking Study ◽  
Moderate Activity ◽  
Molecular Docking Study ◽  
Mass Spectral ◽  
Gram Positive Bacteria ◽  
Ft Ir ◽  
In Silico Molecular Docking

Background: Antimicrobial resistance is major global health problem, which is being rapidly deteriorating the quality of human health. Series of substituted N-(benzo[d]thiazol-2-yl)-2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)acetamide (3a-j) were synthesized from substituted N-(benzo[d]thiazol-2-yl)-2-chloroacetamide/bromopropanamide (2a-j) and 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole (2) and further evaluated for their docking properties and antimicrobial activity. Methods: All synthesized compounds were characterized by FT-IR, NMR and Mass spectral analysis. All compounds were allowed to dock against different antimicrobial targets having PDB ID: 1D7U and against common antifungal target having PDB ID: 1EA1. Results: The compounds 3d and 3h were showed good activity against Methicillin-resistant Staphylococcus aureus (MRSA, resistance Gram-positive bacteria). All synthesized compounds showed good to moderate activity against selected bacterial and fungal microbial strains. If we compared the actual in-vitro antimicrobial activity and in-silico molecular docking study, we found that molecules 3i and 3h were more potent than the others. Conclusion: Our current study would definitely pave the new way towards designing and synthesis of more potent 2-aminobenzothiazoles derivatives.

scholarly journals Microwave-Assisted Synthesis, Characterization, Antimicrobial and Antioxidant Activity of Some New Isatin Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
G. Kiran ◽  
T. Maneshwar ◽  
Y. Rajeshwar ◽  
M. Sarangapani
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Radical Scavenging ◽  
Microwave Assisted Synthesis ◽  
Stable Free Radical ◽  
Ft Ir ◽  
Antimicrobial And Antioxidant Activity ◽  
New Compounds ◽  
Isatin Derivatives

A series of β-Isatin aldehyde-N,N′-thiocarbohydrazone derivatives were synthesized and assayed for theirin vitroantimicrobial and antioxidant activity. The new compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. All the test compounds possessed a broad spectrum of activity having MIC values rangeing from 12.5 to 400 μg/ml against the tested microorganisms. Among the compounds3e,3jand3nshow highest significant antimicrobial activity. The free radical scavenging effects of the test compounds against stable free radical DPPH (α,α-diphenyl-β-picryl hydrazyl) and H2O2were measured spectrophotometrically. Compounds3j,3n,3l, and3e, respectively, had the most effective antioxidant activity against DPPH and H2O2scavenging activity.

ASSESSMENT OF PHYTOCHEMICALS, TOTAL PHENOL, FLAVONOID CONTENT AND IN VITRO ANTIOXIDANT PROPERTY OF LARGE CARDAMOM EXTRACTS

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (10) ◽  
pp. 34-41
Author(s):  
Kanthlal S. K. ◽  
Jipnomon Joseph ◽  
Bindhu P. Paul ◽  
Vijayakumar M ◽  
Rema Shree A. B. ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Antioxidant Property ◽  
Bioactive Constituents ◽  
Preliminary Assessment ◽  
Reducing Power Assay ◽  
Large Cardamom

Amomum subulatum, commonly known as large or black cardamom, is a commonly used spice in Indian kitchens and is traditionally used to treat various ailments. To add more knowledge about the medicinal values of the fruit, this study was conducted to evaluate the in vitro antioxidant activities of aqueous, methanol, ethanol, hydro alcohol, ethyl acetate, acetone and chloroform extracts of the fruit. Preliminary assessment was done to detect the presence of phytoconstituents using identification tests. The antioxidant activity was measured by employing methods such as diphenylpicrylhydrazyl (DPPH) radical scavenging assay, total antioxidant activity equivalent to ascorbic acid, reducing power assay and superoxide anion scavenging assay. The antioxidant activities were compared with their respective phenol and flavonoid contents. Preliminary assessment revealed that large cardamom fruit is a good source of all the bioactive constituents as well as phenol and flavonoid essential for medicinal values. The extract obtained by polar solvents showed the highest antioxidant efficacy in relation to its phenol content. Also, all the solvent-soluble fractions showed a concentration-dependent antioxidant effect. Results from our study prove that large cardamom can alleviate oxidative stress, suggesting the potential of large cardamom as a functional food

scholarly journals Influence of Indole acetic acid and Tryptophan on production of Vinblastine and Vincristine of Catharanthus roseous callus cells in the accumulation media of In Vitro tissue culture

2010 ◽  
Vol 7 (3) ◽  
pp. 1113-1119
Author(s):  
Baghdad Science Journal
Keyword(s):  
Tissue Culture ◽  
High Performance Liquid Chromatography ◽  
Acetic Acid ◽  
Liquid Chromatography ◽  
In Vitro Culture ◽  
High Performance ◽  
Indole Acetic Acid ◽  
Culture Technique

This study on the plant of Ain –AL Bason Catharanthus roseous showed the ability of callus cells that is produced by In Vitro culture technique and transformed to the accumulated media (MS 40gm/L sucrose ,2gm/L IAA Indole acetic acid , 0.5gm/L Tryptophan) to produce Vinblastine and Vincristine compounds. Extraction, purification and quantitive determination of Vinblastine and Vincristine compounds using High performance liquid chromatography technique (HPLC)were carried out. The results showed that the highest concentration of Vinblastine and Vincristine compounds were ( 4.653,12.5 (ppm /0.5 dry Wight respectively from transformed callus cells from MS 40 gm /L sucrose , 2 gm / L NAA Naphthaline acetic acid .

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