scholarly journals DMFDMA catalyzed synthesis of 2-((Dimethylamino)methylene)-3,4-dihydro-9-arylacridin-1(2H)-ones and their derivatives: in-vitro antifungal, antibacterial and antioxidant evaluations

2018 ◽  
Vol 16 (1) ◽  
pp. 1077-1088
Author(s):  
L. Jyothish Kumar ◽  
S. Sarveswari ◽  
V. Vijayakumar

AbstractA series of 3,4-dihydro-9-arylacridin-1(2H)-ones was synthesized and enaminone function was introduced at the C-2 position using DMFDMA catalyst which in turn successfully converted into pyrazole, isoxazol, 1-phenyl-1H-pyrazole by treating it with reagents such as hydrazine, hydroxylamine and phenylhydrazine. These newly synthesized compounds were evaluated for their antibacterial activity against a series of Gram-Positive bacteria including Staphylococcusaureus, Bacilluscereus, StaphylococcusaureusMLS16 and Gram-Negative bacteria including Klebsiellaplanticol, Escherichiacoliand Pseudomonasaeruginosaand also against fungal strains including Candidaalbicans, Candidaparapsilosis, Candidaglabrata, Candidaaaseri, Aspergillusnigerand Issatchenkiahanoiensis. The compounds3aand6aexhibited considerable antifungal activity (MIC value 0.007 and 0.006 μM) against Candidaalbicansand Aspergillusnigerrespectively. The compound4ashowed excellent antibacterial activity towards EscherichiaColi(MIC = 0.003 μM) and the compound5afound to show prominent DPPH radical scavenging activity with EC50value 16.85±1.5μg mL−1.

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (10) ◽  
pp. 38-42
Author(s):  
N. K Choudhary ◽  
◽  
J Dwivedi ◽  
S Sharma

The present investigations were carried out to evaluate the in vitro antioxidant as well as antidiabetic activity of flowers of Calotropis gigantea. Different extracts (petroleum ether, chloroform and ethanolic extract) were prepared using successive solvent extraction method (soxhlet) and screened for its in vitro antioxidant activity using Diphenyl picryl hydrazyl (DPPH) radical scavenging activity, ABT S radical cation decolorization assay and nitric oxide (NO) radical scavenging activity and IC50 were calculated. In vitro antidiabetic activity was studied using α – amylase and α – glucosidase inhibitory assay. Chloroform extract, among the three extracts (i.e. petroleum ether, chloroform and ethanolic), showed maximum antioxidant activity with IC50 value of 151.23µg/ml, 73.56 µg/ml and 158.92µg/ml against DPPH radical scavenging activity, ABTS radical cation decolorization assay and nitric oxide (NO) radical scavenging activity respectively. The chloroform extract produced a significant in vitro antidiabetic activity with IC50 of 52.3µg/ml 18.2µg/ml against α – amylase and α – glucosidase enzymes but less inhibitory effect than standard acarbose.


2020 ◽  
Vol 54 (2 (252)) ◽  
pp. 132-137
Author(s):  
A.G. Simonyan ◽  
R.R. Sargsyan ◽  
H.H. Panosyan ◽  
A.H. Trchounian

Antibacterial and antioxidant activities of different extracts of saxicolous lichen Xanthoparmelia stenophylla sampled from Norashen, Gegharkunik Province of Armenia were studied. Methanol, ethanol and acetone extracts of lichen thalli were demonstrated to have activity against only tested gram-positive bacteria. Methanol extract of the lichen showed the highest amount of DPPH radical scavenging activity (~68%). Our studies did not reveal any significant antibacterial and antioxidant activities of aqueous extract.


Author(s):  
Abdul Sadat ◽  
Mayukh Hore ◽  
Kaushik Chakraborty ◽  
Subhrajyoti Roy

Objective: The present study was carried out to evaluate the in vitro preliminary phytochemical analysis and antioxidant activity of methanolic leaf extracts of Corchorus olitorius L. The in vitro antioxidant activity was evaluated by DPPH radical scavenging activity method.Methods: Fresh jute leaves (immature, mature and senescence) were collected, air dried and the crude powder was prepared for phytochemical and antioxidant analysis. The powder was mixed with 70% methanol and the supernatant was separated. The antioxidant activity of this methanolic extract was measured on the basis of the scavenging activity of the stable 1, 1-diphenyl 2-picrylhydrazyl (DPPH) free radical with slight modifications. Phytochemical analysis was performed according to standard laboratory protocol.Results: The results indicated the presence of different phytochemicals viz. glycosides, steroids, cholesterol, alkaloids, phenols, flavonoids, riboflavin, saponins and terpenoids. The sample also showed antioxidant activity by inhibiting DPPH radical. The significant antioxidant activity of methanolic leaf extract of might be due to the presence of saponins, phenols, flavonoids and alkaloids found in the preliminary phytochemical analysis.Conclusion: Present study reveals that the jute leaf possesses different phytonutrients and exhibited DPPH radical scavenging activity, and therefore, may be used for therapeutic purposes.


Molecules ◽  
2012 ◽  
Vol 17 (12) ◽  
pp. 14882-14898 ◽  
Author(s):  
Francisco Martínez-Martínez ◽  
Rodrigo Razo-Hernández ◽  
Ana Peraza-Campos ◽  
Manuel Villanueva-García ◽  
Maria Sumaya-Martínez ◽  
...  

2016 ◽  
Vol 4 (04) ◽  
pp. 15-18
Author(s):  
Sooad Al-Daihan ◽  
Abeer M Aldbass ◽  
Latifah M Alotebi ◽  
Ramesa Shafi Bhat

Perseaamericana Mill used in traditional medicine for the treatment of various ailments and has antibacterial, antifungal, anti-viral and wound-healing properties. In the present study, antioxidant and antibacterial activity of different extracts of Perseaamericana Mill were investigated. Antioxidant potential of plant extracts was evaluated by means of total phenolic, total flavonoids content and DPPH radical scavenging activity. The highest phenolic and flanovoid content was observed in methanol extract while the lowest was achieved in aqueous extract. At concentration of 500 SOH g/mL, DPPH radical scavenging activity was found to be highest in methanol extract (70%) and lowest in aqueous extract (51%). Antibacterial activity of different extracts was evaluated by using the disk diffusion method. Highest antibacterial activity was observed with methanol extract against S. pyogenes, while minimum activity was observed with aqueous extract against E.coli.


2014 ◽  
Vol 79 (5) ◽  
pp. 517-526
Author(s):  
Maya Chochkova ◽  
Assya Georgieva ◽  
Galya Ivanova ◽  
Nadya Nikolova ◽  
Luchia Mukova ◽  
...  

Seven N-hydroxycinnamoyl amides were synthesized by EDC/HOBt coupling of the corresponding substituted cinnamic acids (p-coumaric-, ferulic-, sinapic- and caffeic acids) with influenza antivirals (amantadine, rimantadine and oseltamivir). DPPH (1,1-diphenyl-2-picrylhydrazyl) scavenging abilities and the inhibitory effect on mushroom tyrosinase activity (using L-tyrosine as the substrate) were investigated in vitro. Amongst the synthesized compounds, N-[(E)-3-(3?,4?-dihydroxyphenyl)-2-propenoyl]oseltamivir (1) and N-[(E)-3-(3?,4?-dihydroxyphenyl)-2-propenoyl]rimantadine (4), containing catechol moiety, exhibited the most potent DPPH radical-scavenging activity. Amide (1) displayed also tyrosinase inhibitory effect toward L-tyrosine as the substrate (~50%). Due to its biological activities revealed so far compound (1) can be considered as a promising candidate for a cosmetic ingredient. The synthesized compounds were also investigated for their in vitro inhibitory activity against the replication of influenza virus A (H3N2).


Foods ◽  
2020 ◽  
Vol 9 (6) ◽  
pp. 694 ◽  
Author(s):  
Seung Yun Lee ◽  
Seung Jae Lee ◽  
Dong Gyun Yim ◽  
Sun Jin Hur

We investigated the effects of in vitro human digestion on the content and bioavailability of onion quercetin and grape resveratrol caused by the composition of saliva or gastric, duodenal, or bile juice. We observed the digestibility of extracted onion quercetin and grape resveratrol, respectively, in the small intestine of the in vitro human digestion system. By liquid chromatography–mass spectroscopy, we found that the degradation of quercetin and resveratrol was influenced by small intestine digestion. Before and after in vitro human digestion, the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities of homogenized water- and ethanol-extracted grapes were higher than those of onion extracts. DPPH radical scavenging activity in both quercetin and resveratrol was decreased by in vitro digestion. These results will improve our understanding of how human digestion influences the contents and free radical scavenging activities of quercetin and resveratrol.


Author(s):  
Mohideen Askar Nawas P ◽  
Sujatha Ravi

Marine algae are known to produce a wide variety of bioactive secondary metabolites and several compounds have been derived from them for prospective development of novel drugs by the pharmaceutical industries. The marine red seaweed Caulacanthusustulatus, collected from the Kilakarai region located between (9.23135° N, 78.7844° E) Ramanathapuram District, Tamil Nadu, India. The seaweed extract was prepared from various solvent extracts namely aqueous, ethanol, methanol and acetone was tested for their phytochemical analysis, antibacterial activity against human pathogens viz., Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus and aquatic pathogens viz., Aeromonas hydrophila and Vibrio vulnificus using disc diffusion methods and in vitro antioxidant activity such as DPPH radical scavenging activity, ABTS radical scavenging activity and Hydroxyl radical scavenging activity of selected solvent extracts. Phytochemical analysis of sixteen different chemical compounds was carried out. The maximum nine phytochemical compounds were present in the methanol and ethanol extracts and the minimum six compounds were present in aqueous extract. The highest antibacterial activity was present in human pathogen P. aeruginosa (20.66 ± 1.1mm) likewise the aquatic pathogen the antibacterial activity was increase in Aeromonas hydrophila (20.33 ± 1.5mm). The methanol extract was significantly higher in DPPH radical scavenging activity (67.07 ± 0.5μg/ml), ABTS radical scavenging activity (72.4 ± 0.6 μg/ml) and Hydroxyl radical scavenging activity (54.06 ± 0.58μg/ml). This study indicates the potential use of red seaweed; in particularC.ustulatus extracts are treating human and aquatic bacterial pathogens and it could be a potential candidate for the natural compounds as antioxidant.


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