Microwave-assisted synthesis, characterization and biological activity of novel pyrazole derivatives

Selvam, Theivendren Panneer; Kumar, Palanirajan Vijayaraj; Govindaraj, Saravanan; Prakash, Chinnasamy Rajaram

doi:10.1016/j.jscs.2011.12.006

Cited by 41 publications

(19 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…COX-1 is responsible for prostaglandins production whereas COX-2 is responsible for the increased production of prostaglandins during in ammation [4]. Inhibition of COX-2 should be speci c as COX-1 inhibition may leads to alter its housekeeping function [5,6].…”

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

View full text Add to dashboard Cite

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.

show abstract

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

View full text Add to dashboard Cite

show abstract

“…In this perspective, nitrogen‐containing heterocyclics have gained much interest in the field of pharmaceutical chemistry . Among them, pyrazoles are usually the core fragment of pharmaceutical drugs such as deracoxib, celecoxib, oxyphenbutazone, phenylbutazone, kebuzone, and feprazone with reduced ulcer genic side effects . Among the pyrazoles, in particular, indeno[1,2‐ c ]pyrazol‐4‐ones are an important class of heterocycles because of pervasiveness of biological activities .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Biological Evaluation, and Molecular Docking Studies of Some N‐thiazolyl Hydrazones and Indenopyrazolones

Mor

Sindhu

Nagoria

et al. 2019

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

Two new series of N‐thiazolyl hydrazones (3a–h) and indenopyrazolones (4a–h) were synthesized by the reaction of various 2‐acyl‐(1H)‐indene‐1,3(2H)‐diones, thiosemicarbazide, and phenacyl bromide/substituted phenacyl bromides. The in vitro antimicrobial activity of these synthesized compounds was assayed against four bacteria, namely, Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa, and two fungi, namely, Candida albicans and Aspergillus niger, by employing serial dilution method. Ciprofloxacin and fluconazole were used as antibacterial and antifungal reference drugs, respectively. Results of antimicrobial assay showed that the tested compounds have broad range of activity. The compounds 3h and 4a against C. albicans displayed more potency than fluconazole whereas 3b and 3c against B. subtilis showed activity comparable with ciprofloxacin. The synthesized indenopyrazolones (4a–h) were evaluated for their in vitro antioxidant activity by 2,2‐diphenyl‐1‐picrylhydrazyl radical scavenging assay using ascorbic acid as reference. Compound 4b exhibited the highest 2,2‐diphenyl‐1‐picrylhydrazyl radical scavenging with IC50 value 33.14 μg/mL. The observed results of antimicrobial activity were supported by molecular docking study performed to understand the binding interaction of hydrazones (3a–h) and indenopyrazolones (4a–h) with lanosterol 14α‐demethylase.

show abstract

“…The plenteous literature affirms the ubiquitous nature of aza-heterocyclic compounds especially the pyrazole derivatives. They are documented to possess anti-inflammatory [4][5][6][7], antibacterial, antifungal [8][9][10][11], antiviral [12,13], antimalarial [14,15], analgesic [16][17][18], antipyretic [19,20], antidepressant [21][22][23], anticonvulsant [24,25], antidiabetic [26,27], antiangio-genetic [28], antitubercular [29] and anticancer [30][31][32][33] activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Anti-inflammatory, Analgesic and Antipyretic Activity of Novel 1,3,5-Trisubstituted Pyrazole Derivatives

Thatavarthi

Kamal

2019

Asian J. Chem.

View full text Add to dashboard Cite

A novel series of 1,3,5-trisubstituted pyrazole derivatives were synthesized by the cycloaddition reaction between the electron rich N-substituted aryl hydrazones and nitro-olefins. Different N-substituted aryl hydrazones (1a-j) on reacting with 4-methyl-β-nitrostyrene (2) in ethylene glycol or trifluoroethanol-trifluoro acetic acid mixture (for acid stable hydrazones) at 120 ºC, yielded various 1,3,5-trisubstituted pyrazoles (3a-j). The final products were characterized by spectral analysis using Mass, NMR and IR spectroscopy. All the products were assessed for their anti-inflammatory, analgesic and antipyretic activities on Swiss albino rats. All the compounds (3a-j) exhibited noteworthy defence against inflammation, nociception and hyperthermia. Compounds (3e and 3h) disclosed better antiinflammatory, analgesic and antipyretic activities while compound 3c had highest anti-inflammatory activity compared to the standard nimesulide.

show abstract

Microwave-assisted synthesis, characterization and biological activity of novel pyrazole derivatives

Cited by 41 publications

References 15 publications

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

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

Synthesis, Biological Evaluation, and Molecular Docking Studies of Some N‐thiazolyl Hydrazones and Indenopyrazolones

Synthesis, Anti-inflammatory, Analgesic and Antipyretic Activity of Novel 1,3,5-Trisubstituted Pyrazole Derivatives

Contact Info

Product

Resources

About