Synthesis, Antioxidant and Antidiabetic Activity of 1-[(5-Substituted phenyl)-4,5-dihydro-1H-pyrazol-3-yl]-5-phenyl-1H-tetrazole

Kaushik, Niranjan; Kumar, Nitin; Kumar, Anoop

doi:10.4172/pharmaceutical-sciences.1000125

Cited by 15 publications

(4 citation statements)

References 35 publications

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“…All titled molecules were selected for their in vitro antioxidant potential by scavenging of DPPH free radical (Kaushik et al, 2016). Standard ascorbic acid and synthesized compounds were prepared in different concentrations from 10 to 50 µg/ml from the stock solution (100µg/ml) with distilled carbinol.…”

Section: In Vitro Antioxidant Activity Dpph Free Radical Scavenge Actmentioning

confidence: 99%

Synthesis of some novel 3- (4-ethoxyphenyl) -5- (4-substituted) -4,5-dihydro-1H-pyrazole derivatives as potent antioxidant agents

Lakshminarayanan¹,

Kannappan

Subburaju³

et al. 2020

ijrps

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Pyrazolines are the most useful heterocyclic moiety in Pharmaceutical and Chemical ields and as the most potential molecules for the design of new chemical entities. Nitrogen-containing heterocyclic compounds, pyrazolines and their derivatives showed a variety of pharmacological activities, including antioxidant properties. In the present study, eleven novel ethoxylated pyrazoline derivatives were synthesized by condensing chalcones with electron releasing ethoxy group at one end and different electron-donating, electronwithdrawing groups in another end with hydrazine hydrate and alcohol. The compounds synthesized were structural elucidated by their spectroscopic studies. All the compounds synthesized were evaluated for their in vitro antioxidant potential by 2,2'-diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxide free radical scavenging assay methods. Some of these molecules possess moderate to good antioxidant activity when compared to standard ascorbic acid. The compound with methoxy group (EH2) exhibits potent antioxidant activity with IC 50 value of 9.02 and 9.44µg/ml in DPPH and hydrogen peroxide assay methods respectively and the compound with hydroxy group (EH9) also showed potent antioxidant activity with IC 50 value of 12.41 and 14.56µg/ml in DPPH and hydrogen peroxide free radical scavenging assay methods respectively when compared to standard. The compounds containing electron-donating substituents were found to be good antioxidants when compared to standard ascorbic acid.

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Section: In Vitro Antioxidant Activity Dpph Free Radical Scavenge Actmentioning

confidence: 99%

Synthesis of some novel 3- (4-ethoxyphenyl) -5- (4-substituted) -4,5-dihydro-1H-pyrazole derivatives as potent antioxidant agents

Lakshminarayanan¹,

Kannappan

Subburaju³

et al. 2020

ijrps

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“…It has been indicated that increase in blood glucose level cause oxidative stress which may add up in the pathogenesis of further diabetic complications. Oxidative stress, occurs due to increase in free radical concentration, damages various organs and affecting normal biological functioning [3].…”

Section: Persistent Increase In Blood Glucose Level Leads To Diabetesmentioning

confidence: 99%

Design, Synthesis, in Vitro Antioxidant, Anti-Inflammatory and Antidiabetic Evaluation of New N-Substitutedbenzylidene-5-(4-Formylphenyl)-(3-Hydroxyphenyl)-4,5-Dihydropyrazole-1-Carbothioamide Derivatives

Singh¹,

sT²,

pk³

2020

Preprint

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A series of N-substitutedbenzylidene-5-(4-formylphenyl)-(3-hydroxyphenyl)-4,5-dihydropyrazole-1-carbothioamide derivatives was designed, synthesized and examined for their therapeutical potential against prooxidant (oxidative stress), inflammation and diabetes. Biological results showed antioxidant activity with IC50 value 37.68 mol/L, anti-inflammatory activity with IC50 value 26.40 mol/L and antidiabetic activity with IC50 value 17.12 mol/L. The results of antioxidant activity showed that compounds Y9 and Y17 exhibited excellent antioxidant activity with IC50 values 17.43 mol/L and 18.98 mol/L, results of anti-inflammatory activity showed that compounds Y2, Y3 and Y7 exhibited excellent anti-inflammatory activity with IC50 values 23.23 mol/L, 22.09 mol/L and 19.05 mol/L respectively and results of antidiabetic activity showed that compounds Y1, Y5and Y6 exhibited excellent antidiabetic activity with IC50 values 17.08 mol/L, 8.36 mol/L and 13.50 mol/L. When compared with ascorbic acid, aspirin and acarbose as standard drug respectively. Heterocyclic compounds have diversity in their structure which makes them broad and economical therapeutic agents. Pyrazole is a five membered ring containing three carbon and two neighboring nitrogen atoms. Pyrazole and its derivatives have various biological as well as clinical potential thus considered for further research. Due to wide range of therapeutical activities pyrazole makes interest among researcher to explore it further for more activities. Pyrazole is present in various biological moieties eg. antimicrobial, antidiabetic, anti-inflammatory, antioxidant, antiviral, anticonvulsant, anticancer, anti-HIVand anti-tuberculosis agents.

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“…The synthetic procedure and spectral characterisation of synthesised compounds described in earlier reports by author [24,25]. The equal quantity of sodium azide, ammonium chloride and benzonitrile were refluxed with dimethylformamide at 125 °C for 7-8 hours, the reaction mixture was poured in 100 ml of water; a milky solution was obtained which was acidified with concentrated hydrochloric acid to get the precipitate.…”

Section: General Procedures For the Synthesis Of 5-phenyl Tetrazolementioning

confidence: 99%

Anticancer and Molecular Docking Studies of 1-(5-substituted phenyl) isoxazol-3-yl)-5-phenyl-1H-tetrazoles

Kaushik

Kumar

et al. 2019

IJBcRR

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Cancer a leading cause of human mortality worldwide is characterised by the unseemly growth of cellular mass and signalled through the enlargement of stress. Management of cancer treatment is still buried and has been recently alerting the need to discover a drug molecule with lesser side effects. The objective of the present study is to explore the anticancer activity and docking studies of 1-(5-substituted phenyl) isoxazol-3-yl)-5-phenyl-1H-tetrazole derivatives. The compounds were evaluated for in-vitro anticancer activity under the drug discovery program of National Cancer Institute (NCI), USA. Only seven compounds were selected and screened for anticancer activity at a single high dose (10-5 M) using NCI 60 cancer cell lines. Among all the selected compounds, 4b and 4i exhibited significant anticancer activity against Leukemia cell lines. Molecular docking studies for the 5-phenyl-1-(5-substituted phenylisoxazol-3-yl)-1H-tetrazole analogues was done by Schrodinger software. Docking results stated that the compounds 4b and 4i has good dock score among the other derivatives which shows good binding efficiency towards receptor.

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Synthesis, Antioxidant and Antidiabetic Activity of 1-[(5-Substituted phenyl)-4,5-dihydro-1H-pyrazol-3-yl]-5-phenyl-1H-tetrazole

Cited by 15 publications

References 35 publications

Synthesis of some novel 3- (4-ethoxyphenyl) -5- (4-substituted) -4,5-dihydro-1H-pyrazole derivatives as potent antioxidant agents

Synthesis of some novel 3- (4-ethoxyphenyl) -5- (4-substituted) -4,5-dihydro-1H-pyrazole derivatives as potent antioxidant agents

Design, Synthesis, in Vitro Antioxidant, Anti-Inflammatory and Antidiabetic Evaluation of New N-Substitutedbenzylidene-5-(4-Formylphenyl)-(3-Hydroxyphenyl)-4,5-Dihydropyrazole-1-Carbothioamide Derivatives

Anticancer and Molecular Docking Studies of 1-(5-substituted phenyl) isoxazol-3-yl)-5-phenyl-1H-tetrazoles

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