Synthesis, Characterization and antioxidant activities of Semicarbazide and Thiosemicarbazide Derivatives

2021 ◽  
Vol 43 (4) ◽  
pp. 475-475
Author(s):  
Abdul Manaf Abdul Manaf ◽  
Momin Khan Momin Khan ◽  
Khair Zaman Khair Zaman ◽  
Mahboob Ali Mahboob Ali ◽  
Faima Alam Faima Alam ◽  
...  

In this research work Semicarbazide, thiosemicarbazide derivatives 3 to 25 were synthesized by conventional methods with high percentage yield and reaction rate. 1H-NMR and EIMS spectroscopic techniques were used to elucidate the structure of the synthesized compounds. The effect of thiosemicarbazide and semicarbazide derivatives as an antioxidant agents were studied by DPPH free radical scavenging, ferric ion reducing, ferrous ion chelating assays. Higher DDPH radical scavenging activity exhibited by most of the compounds as compared to standard vitamin C. Excellent ferric ion reducing activity was indicated by compounds of theseriesas compared to standard vitamin C. However most of the compounds generally showed average ferrous ion chelating activity than standard EDTA.

2019 ◽  
Vol 16 (3) ◽  
pp. 249-255
Author(s):  
Momin Khan ◽  
Umar Ali ◽  
Anis Ur Rahman ◽  
Muhammad Ibrahim ◽  
Abdul Hameed ◽  
...  

Background: The role of small molecules as antioxidants to prevent the oxidation of other molecules and inhibit them from radical formation is the area of much interest to cure disease especially cancer. Moreover, the antioxidants play important role as stabilizers to prevent oxidation of fuels and lubricants. </P><P> Methods: In the present study, fifteen tetrakis-Schiff’s bases derivatives (1-15) were synthesized and screened for their antioxidant activities. Compounds 1-15 were synthesized by continuous stirring of reaction mixture of 1,4-bis (hydrazonomethyl)benzene (1 mmol) with various substituted aromatic aldehydes (2 mmol) in distilled water using acetic acid as catalyst at room temperature for 2-10 min. </P><P> Results: Our present study showed that all compounds are better ferrous ion-chelating agents except compound 1,4-bis((E)-((E)-(3,4-dimethoxybenzylidene)hydrazono)methyl)benzene (6) (IC50 = 329.26 &#177; 4.75 &#181;M) which has slightly low activity than the standard EDTA (IC50 = 318.40 &#177; 5.53 μM). In addition, DPPH radical scavenging activity of eleven compounds showed higher activity than the standard. However, remaining four compounds showed comparable radical scavenging activity to the standard DPPH (IC50 = 257.77 &#177; 4.60 &#181;M). </P><P> Conclusion: The series of fifteen Schiff’s bases (1-15) were synthesized and evaluated as antioxidants. From both assays, it has been demonstrated that most of the tetrakis-Schiff’s bases have potential to serve as leads for the development of antioxidant agents for future research.


2020 ◽  
Vol 10 (3) ◽  
pp. 312-321
Author(s):  
Idin Sahidin ◽  
Carla W. Sabandar ◽  
Wahyuni ◽  
Rini Hamsidi ◽  
Sandra Aulia Mardikasari ◽  
...  

Background: Marine sponges provided a great source of natural products with promising biological activity. This study was aimed to investigate the chemical constituents of methanol extracts of selected Indonesian marine sponges (Callyspongia sp., Clathria sp., Melophlus sarasinorum, and Xestospongia sp.), collected from the Saponda Islands, Southeast Sulawesi, Indonesia as well as to evaluate their antimicrobial and antioxidant activities. Methods: LCMS/MS analysis used to identify the compounds. Agar well diffusion and DPPH assays were used to evaluate the antimicrobial and antioxidant activities. Results: Chemical screening reported alkaloids, terpenoids, steroids, and saponins from all investigated sponges. The LC-MS/MS analysis identified various compounds which mainly contained steroids. Antimicrobial activity (against Bacillus subtilis, Escherichia coli, Salmonella enterica, and Candida albicans) was only shown by the Xestospongia sp. extract. Meanwhile, extracts of M. sarasinorum, Xestospongia sp., and Callyspongia sp. exhibited potent radical scavenging activity. Conclusion: The study concluded that the selected sponges could provide various groups of compounds. Methanol extracts of these sponges could be used as sources of antimicrobial and antioxidant agents.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Mehdi Farshad Ashraf ◽  
Maheran Abd Aziz ◽  
Johnson Stanslas ◽  
Ismanizan Ismail ◽  
Mihdzar Abdul Kadir

The present paper focused on antioxidant and cytotoxicity assessment of crude and total saponin fraction ofChlorophytum borivilianumas an important medicinal plant. In this study, three different antioxidant activities (2,2-diphenyl-1-picrylhydrazyl radical scavenging (DPPH), ferrous ion chelating (FIC), andβ-carotene bleaching (BCB) activity) of crude extract and total saponin fraction ofC. borivilianumtubers were performed. Crude extract was found to possess higher free radical scavenging activity (ascorbic acid equivalents 2578 ± 111 mg AA/100 g) and bleaching activity (IC50= 0.7 mg mL−1), while total saponin fraction displayed higher ferrous ion chelating (EC50= 1 mg mL−1). Cytotoxicity evaluation of crude extract and total saponin fraction against MCF-7, PC3, and HCT-116 cancer cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) cell viability assay indicated a higher cytotoxicity activity of the crude extract than the total saponin fraction on all cell lines, being most effective and selective on MCF-7 human breast cancer cell line.


2010 ◽  
Vol 5 (3) ◽  
pp. 338-345 ◽  
Author(s):  
Mohammad Ebrahimzadeh ◽  
Seyed Nabavi ◽  
Seyed Nabavi ◽  
Bahman Eslami

AbstractAntioxidant activity of the aerial part and bulbs of Allium paradoxum was investigated by eight in vitro assay systems. Extracts showed good antioxidant activity. IC50 for 1,1-diphenyl-2-picryl hydrazyl radical-scavenging activity was 890.9±43.2 and 984.9±33.5 µg/ml for the aerial part and bulbs, respectively. The aerial parts have better reducing power than bulb extracts but not comparable with Vitamin C (P>0.001). Extracts showed weak Fe2+ chelating ability, the IC50 being 959±47 and 530±24 µg/ml for bulbs and aerial parts, respectively. Both tested extracts exhibited good hydrogen peroxide scavenging in a concentration dependent manner. They exhibited good antioxidant activity against the hemoglobin-induced linoleic acid system that was comparable with vitamin C (P>0.01). They showed good activity against cumene hydro peroxide induced hemolysis in RBCs. In addition, they possessed antihemolytic activity. The extract from aerial parts had significantly higher total phenol and flavonoid content than did bulbs. Amounts of eight elements (Cu, Mn, Zn, Fe, Ni, Pb, Cd and Cr) were also determined in the bulb and aerial part using atomic absorption spectroscopy. They contained higher Fe and Mn contents than other elements.


Author(s):  
Bharat B. Kashid ◽  
Jaydeo T. Kilbile ◽  
Kishor D. Wani ◽  
Suhas. M. Pawar ◽  
Vijay M. Khedkar ◽  
...  

Objective: The research work aims synthesis of novel series of hydrazones, antioxidant screening, evaluate the binding affinities, and in silico methods for the identification of possible drug targets of synthesized compounds. Methods: This report briefly explains the synthesis of novel series of hydrazones was synthesized via. hydrazinolysis of esters to obtain hydrazide, treated with aldehyde and acetophenone to get hydrazones. The spectral confirmed hydrazones exhibited excellent to comparable anti-oxidant as compaired to the standard drugs Butylated hydroxytoluene (BHT) and Ascorbic acid. Molecular docking on myeloperoxidase (MPO) demonstrated the ability of this scaffold to correctly recognize the target and engage in significant bonded and non-bonded interactions with key residues therein. Results and Discussion: In this study, we report an effectively synthesized compounds BK-35, BK-41, BK-26, BK-28 and BK-39 showed the best DPPH radical scavenging activity. The docking results clearly showed the binding mode of hydrazones into the active site of Myeloperoxidase (MPO). An in-silico results, no any of the synthesized compounds BK24 to BK-41 violated Lipinski’s rule of five (miLog P ≤ 5). Conclusions: In vitro preliminary antioxidant screening results in support by in Silico binding affinity data of novel hydrazones of levofloxacin related molecules BK-24 to BK-41 reported here have emerged as excellent antioxidant agents. The inference derived from the in vitro antioxidant screening data and the quantitative insights derived from the per-residue interaction analysis with MPO enzyme, are now being fruitfully utilized for site specific mutation around the nucleus to identify selective and potent antioxidants.


2020 ◽  
Vol 7 (3) ◽  
pp. 222-229
Author(s):  
Syed Tajudeen Syed Ameen ◽  
Anbalagan Vilvanathan ◽  
Syed Zameer Ahmed Khader ◽  
Gayathri Mahalingam

Background: A series of β-diketone hydrazones have been synthesized via condensation of isoniazid with series of β-diketone. The structures of the Schiff bases are established by elemental and spectroscopic techniques. The prepared compounds were screened for antibacterial and antioxidant potential by DPPH free-radical scavenging activity and Ferric reducing antioxidant power (FRAP) assays. Methods: β-diketone hydrazine derivatives were synthesized by simple condensation between various β-diketones and isoniazid. The titled compounds were synthesized following both conventional and microwave irradiation methods. The in vitro antibacterial activity of synthesized derivatives was evaluated against gram-positive (B. subtilis, S. aureus and S. pyogenes) and gram-negative (E. coli, and K. pneumonia) bacterial strains and expressed in terms of zone of inhibition and also screened for antioxidant activity. Results: The yield of products was appreciably increased in shorter reaction times with the aid of microwave-assisted synthesis. Therefore, it follows the green chemistry approach by making the above reactions eco-friendly. The synthesized compounds were characterized using FT-IR, 1H NMR, 13C NMR, and elemental analysis techniques. The spectroscopic techniques showed the formation of β-diketone hydrazone compounds. Theoretical data show good agreement with the experimental results. Some of the compounds displayed significant antibacterial and antioxidant potentials when compared to the standard drug. Conclusion: In the present research work, we report the synthesis of some novel β-diketone hydrazone derivatives. A high yield of compounds was noted under microwave-assisted reaction in shorter reaction times. The results revealed that the synthesized Schiff bases showed good radical scavenging activity.


2016 ◽  
Vol 11 (2) ◽  
pp. 301 ◽  
Author(s):  
Maroua Akacha ◽  
Karima Lahbib ◽  
Néziha Ghanem Boughanmi

<p>Phytotherapy is a discipline which is interested in the design, the preparation and the interpretation of structure activity relationship of the natural bioactive molecules. In this context, ethanolic leaves extract of <em>Melia azedarach</em> L. was phytochemically analysed on the bases of HPLC and by GC–MS. Extract wase tested for his in vitro antioxidant activities by 1,1-diphenyl-2-picrylhydrazyl (DPPH), H<sub>2</sub>O<sub>2</sub>, hydroxyl radical scavenging activity, Ferric Reducing Power (FRP) and Ferrous ion chelating abilities methods. The antioxidant activity of the extract was analyzed simultaneously with their pro-oxidant capacity. The ratio of pro-oxidant to the antioxidant activity (ProAntidex) represents a useful index of the net free radical scavenging potential of the synthesized compounds. Tested extract showed significant antioxidant activity with a moderate ProAntidex.</p><p><strong>Video clips:</strong></p><p><a href="https://youtube.com/v/FkqJ-qAoyNI">Ferrous ion chelating ability (FIC) 1</a></p><p><a href="https://youtube.com/v/LiZIYq54-ms">Ferrous ion chelating ability (FIC) 2</a></p><p><a href="https://youtube.com/v/dTNWTEQf8Hs">Ferrous ion chelating ability (FIC) 3</a></p><p> </p>


Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1205
Author(s):  
Adesola A. Adeleke ◽  
Sizwe J. Zamisa ◽  
Md. Shahidul Islam ◽  
Kolawole Olofinsan ◽  
Veronica F. Salau ◽  
...  

A series of fifteen silver (I) quinoline complexes Q1–Q15 have been synthesized and studied for their biological activities. Q1–Q15 were synthesized from the reactions of quinolinyl Schiff base derivatives L1–L5 (obtained by condensing 2-quinolinecarboxaldehyde with various aniline derivatives) with AgNO3, AgClO4 and AgCF3SO3. Q1–Q15 were characterized by various spectroscopic techniques and the structures of [Ag(L1)2]NO3Q1, [Ag(L1)2]ClO4Q6, [Ag(L2)2]ClO4Q7, [Ag(L2)2]CF3SO3Q12 and [Ag(L4)2]CF3SO3Q14 were unequivocally determined by single crystal X-ray diffraction analysis. In vitro antimicrobial tests against Gram-positive and Gram-negative bacteria revealed the influence of structure and anion on the complexes′ moderate to excellent antibacterial activity. In vitro antioxidant activities of the complexes showed their good radical scavenging activity in ferric reducing antioxidant power (FRAP). Complexes with the fluorine substituent or the thiophene or benzothiazole moieties are more potent with IC50 between 0.95 and 2.22 mg/mL than the standard used, ascorbic acid (2.68 mg/mL). The compounds showed a strong binding affinity with calf thymus-DNA via an intercalation mode and protein through a static quenching mechanism. Cytotoxicity activity was examined against three carcinoma cell lines (HELA, MDA-MB231, and SHSY5Y). [Ag(L2)2]ClO4Q7 with a benzothiazole moiety and [Ag(L4)2]ClO4Q9 with a methyl substituent had excellent cytotoxicity against HELA cells.


2019 ◽  
Vol 11 (1) ◽  
pp. 144-148
Author(s):  
Aicha Bouhafsoun ◽  
Mehmet Boga ◽  
Ahmed Boukeloua ◽  
Hamdi Temel ◽  
Meriem Kaid-Harche

The present study was carried out to investigate the antioxidant activity of the water and methanol extracts of leaves and fruits extracts of Chamaerops humilis L. by using ABTS cation radicals and cupric reducing antioxidant capacity (CUPRAC). Anticholinesterase effect of the extracts was tested against both AChE and BChE using a microplate-reader assay based on the Ellman method. The methanol extracts of C. humilis leaves contained relatively higher content of flavonoids and total phenolics than those of fruits. All the extracts were found to have different levels of antioxidant activity in the systems tested. The leave extract showed the highest value of antioxidant activity, based on ABTS radical-scavenging activity, while the fruit water extract showed the highest value (0.53±0.50 µg/mL) of cupric reducing antioxidant activity.  Our data indicates that both methanol and water fruit extract were active for BChE inhibition (31.65 ± 0.37 and 30.19 ± 0.56%) respectively, whereas, all leave extracts did not show any activity against BChE. The present study demonstrated that the methanol and water extracts fractions of C. humilis have different responses with different antioxidant methods. Our results suggest that the C. humilis could be used as a source of antioxidant agents and may be beneficial in the AD treatment.


2020 ◽  
Vol 14 (1) ◽  
pp. 58-68
Author(s):  
Dattatraya G. Raut ◽  
Sandeep B. Patil ◽  
Prafulla B. Choudhari ◽  
Vikas D. Kadu ◽  
Anjana S. Lawand ◽  
...  

Background: The present research work is focused on the development of alternative antioxidant and anti-inflammatory agents. The review of the literature reveals that many benzofused thiazole analogues have been used as lead molecules for the design and development of therapeutic agent, including anticancer, anti-inflammatory, antioxidant and antiviral. The synthesized benzofused thiazole derivatives are evaluated for in vitro antioxidant, anti-inflammatory activities and molecular docking study. Thus, the present research work aims to synthesize benzofused thiazole derivatives and to test their antioxidant and antiinflammatory activities. Objective: To design and synthesize an alternative antioxidant and anti-inflammatory agents. Methods: The substituted benzofused thiazoles 3a-g were prepared by cyclocondensation reaction of appropriate carboxylic acid with 2-aminothiophenol in POCl3 and heated for about 2-3 h to offer benzofused thiazole derivatives 3a-g. All the newly synthesized compounds were in vitro screened for their anti-inflammatory and antioxidant activities by using a known literature method. Results: At the outset, the study of in vitro indicated that the compounds code 3c, 3d and 3e possessed distinct anti-inflammatory activity as compared to a standard reference. All the tested compounds show potential antioxidant activity against one or more reactive (H2O2, DPPH, SO and NO) radical scavenging species. Additionally, docking simulation is further performed to the position of compounds 3d & 3e into the anti-inflammatory active site to determine the probable binding model. Conclusion: New anti-inflammatory and antioxidant agents were needed; it has been proved that benzofused thiazole derivatives were 3c, 3d and 3e constituted as an interesting template for the evaluation of new anti-inflammatory agents and an antioxidant’s work also may provide an interesting template for further development.


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