Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents

Datar, Prasanna A.; Jadhav, Sonali R.

doi:10.1155/2015/670181

Cited by 24 publications

(18 citation statements)

References 19 publications

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“…Halogenated pyrazolones displayed bioactivities as a potent catalytic inhibitor of human telomerase [52] and as fungicide [53]. Pyrazolones have also been shown anti-HIV [54], anti-diabetic [55], anti-hyperlipidemic [56] and immunosuppressive activity [57].…”

Section: Pharmacological Activities Of Pyrazolones Derivativesmentioning

confidence: 99%

Approaches for Chemical Synthesis and Diverse Pharmacological Significance of Pyrazolone Derivatives: A Review

Asif

2021

J. Chil. Chem. Soc.

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Pyrazolone is a five-membered lactam ring containing two Nitrogens and one ketonic group in its structure. Numerous pyrazolone derivatives were exhibited with diverse biological, pharmacological, and chemical applications. When pyrazolones were discovered, they were only known as NSAIDs but in recent times they play a versatile role in several complications like cerebral ischemia, cardiovascular diseases, antibacterial, antioxidant, anticancer and several other pharmacological activities. Over the last few decades, pyrazolone derivatives have been used for various biochemical applications. Some of these derivatives such as metamizole, phenazone, aminopyrine, and propyphenazone, are widely used as anti-inflammatory and analgesics. The chemistry of pyrazolone has gained increasing attention due to its diverse pharmacological properties such as anticancer, analgesic, anti-inflammatory, antimicrobial, antioxidant, antifungal, antiviral, antidiabetic, and several other biological activities. Thus, keeping because of their importance, synthetic strategies for existing as well as novel pyrazolone derivatives have been developed and explored their biochemical utility. This review deals with the various pharmacological properties of different pyrazolone derivatives and puts chemical synthetic schemes.

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Section: Pharmacological Activities Of Pyrazolones Derivativesmentioning

confidence: 99%

Approaches for Chemical Synthesis and Diverse Pharmacological Significance of Pyrazolone Derivatives: A Review

Asif

2021

J. Chil. Chem. Soc.

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“…The non-competitive inhibitors (1 and 3) are top in the ranking (low binding energy values, E bind ) followed by the competitive compounds (2, 4 and 5). Compound 3 shows the lowest E bind value (-5.15 kcal/mol) indicating the highest binding affinity (Datar & Jadhav 2015) towards NS2B-NS3 Yang et al (2007). 1 = Pinostrobin; 2 = 4-hydroxypanduratin A; 3 = Doxycycline; 4 = Meclofenamic acid; 5 = Rolitetracycline.…”

Section: Scoring Functionmentioning

confidence: 99%

Molecular Docking Studies of Selected Medicinal Drugs as Dengue Virus-2 Protease Inhibitors

Othman¹,

Othman²,

Baharuddin³

et al. 2017

JSM

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Dengue is a potentially deadly disease with no effective drug. An in silico molecular docking was performed using Autodock 4.2.6 to investigate the molecular interactions between protease inhibitors, comprising antibiotic derivatives namely doxycycline (3), rolitetracycline (5) and a non-steroidal anti-inflammatory drug (NSAID), meclofenamic acid (4), against the NS2B-NS3 protease from dengue virus-2 (DENV-2). The non-competitive inhibitor (3) showed lower binding energy (-5.15 kcal/mol) than the predicted competitive inhibitors 4 and 5 (-3.64 and -3.21 kcal/mol, respectively (-5.15 kcal/mol) berbanding sebatian 4 dan 5 (masing-masing -3.64 dan -3.21 kcal/mol). Analisis struktur menunjukkan sebatian 3 yang terikat pada kawasan alosterik, berinteraksi dengan Lys74, iaitu residu asid amino yang terikat dengan salah satu daripada residu triad pemangkinan, Asp75. Sebatian 4 dan 5 pula menunjukkan ikatan langsung dengan dua triad pemangkinan iaitu His51 dan Ser135, justeru diramalkan sebagai perencat kompetitif. Kata kunci: Mengedok; perencat; Denggi adalah sejenis penyakit yang boleh membawa maut dan sehingga kini tiada sebarang ubat untuk merawat penyakit tersebut. Mengedok molekul secara in silico menggunakan Autodock 4.2.6 telah dijalankan untuk mengkaji interaksi molekul antara perencat protease yang terdiri daripada derivatif antibiotik iaitu doxycycline (3) dan rolitetracycline (5) dan dadah anti-radang bukan steroid (NSAID), asid meklofenamik (4), terhadap NS2B-NS3 daripada virus denggi-2 (DENV-2). Perencat tidak-kompetitif (3) menunjukkan tenaga ikatan yang lebih rendah

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“…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.

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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.

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Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents

Cited by 24 publications

References 19 publications

Approaches for Chemical Synthesis and Diverse Pharmacological Significance of Pyrazolone Derivatives: A Review

Approaches for Chemical Synthesis and Diverse Pharmacological Significance of Pyrazolone Derivatives: A Review

Molecular Docking Studies of Selected Medicinal Drugs as Dengue Virus-2 Protease Inhibitors

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

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