Synthesis, biological evaluation and molecular modeling study of pyrazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents

Tewari, Ashish Kumar; Singh, Ved Prakash; Yadav, Pawan Kumar; Gupta, Garima; Singh, Amit; Goel, Raj Kumar; Shinde, Pravin V.; Mohan, C. Gopi

doi:10.1016/j.bioorg.2014.05.004

Cited by 83 publications

(40 citation statements)

References 51 publications

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“…These derivatives show broad spectrum activity such as anti-in ammatory [1], anti-oxidant [2], antipyretic [3], antimicrobial [4], antiviral [5], anticancer [6], antitumor [7], anticonvulsant [8], analgesic [9], antidepressant [10], insecticides and fungicides [11,12]. For this title structure, the asymmetric unit contains two independent molecules ( gure).…”

Section: Discussionmentioning

confidence: 99%

Crystal structure of N′-(4-(dimethylamino)benzylidene)-5-phenyl-1H-pyrazole-3-carbohydrazide, C₁₉H₁₉N₅O

Karrouchi¹,

Radi

Ansar

et al. 2016

Zeitschrift Für Kristallographie - New Crystal Structures

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Section: Discussionmentioning

confidence: 99%

Crystal structure of N′-(4-(dimethylamino)benzylidene)-5-phenyl-1H-pyrazole-3-carbohydrazide, C₁₉H₁₉N₅O

Karrouchi¹,

Radi

Ansar

et al. 2016

Zeitschrift Für Kristallographie - New Crystal Structures

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“…The pyrazole moiety is a good template for designing and developing diverse therapeutic drugs because they are reported to enhance numerous biological properties such as anti‐hyperglycemic, analgesic, antiinflammatory, antipyretic, antibacterial, hypoglycemic and sedative‐hypnotic activities . Synthetic pyrazole based drugs utilized extensively in the pharmaceutical industry include Acomplia ( 1 ), Celebrex ( 2) and Viagra ( 3 ) (Figure ) …”

Section: Introductionmentioning

confidence: 99%

Synthesis of Fused Indolo‐Pyrazoles and Their Antimicrobial and Insecticidal Activities against Anopheles arabiensis Mosquito

2020

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A new approach was used for the synthesis of novel fused indolo‐pyrazoles (FIPs). Indole, arylhydrazine and benzaldehyde derivatives were used for the [3+2] annulation reaction in one‐pot system. The compounds were characterised by 1H NMR, 13C NMR, 2D NMR, MS and elemental analysis. The in vitro antifungal activity of the FIPs were evaluated against Candida albicans, Candida utilis, Saccharomyces cerevisiae, Aspergillus flavus and Aspergillus niger. Two FIPs, viz. N‐methyl‐3‐phenyl‐2, 3‐dihydropyrazolo [3, 4‐b] indole‐1(4H)‐carbothioamide (8 r) and 3‐(4‐methoxyphenyl)‐N‐methyl‐2,3‐dihydropyrazolo[3,4‐b]indole‐1(4H)‐carbothioamide (8 x) displayed good antifungal activity against Saccharomyces cerevisiae with a zone of inhibition diameter of 23 and 20 mm, respectively. They also displayed substantial potency against Saccharomyces cerevisiae with the MIC of 0.18 μM. All FIPs were screened for larvicidal and insecticidal properties against Anopheles arabiensis of which 12 FIPs produced more than 80 % larvae mortality at a 4 μg/mL dose in 24 hours whilst 8 FIPs showed a knock‐down of mosquitoes within the first 60 minutes of exposure, which was comparable to the positive control Temephos.

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“…A famous example of aromatic heterocyclics contains two nitrogen atoms in the five‐membered rings are pyrazoles . Pyrazole derivatives act as monoamine oxidase inhibitors , BRAF inhibitors , DNA gyrase inhibitor , antileishmanial , antiproliferative , anti‐inflammatory , analgesic , and cyclin‐dependent kinase inhibitors (Fig. ).…”

Section: Introductionmentioning

confidence: 99%

The Novel Synthesis of Functionalized Indenopyrazolones Using Fe₃O₄ nanoparticles stabilized on MMT: An Efficient Magnetically Recoverable Heterogeneous Nanocomposite Catalyst

Nasab

Safari

2019

Journal of Heterocyclic Chem

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A practical and simple approach for the one‐pot multicomponent synthesis of indenopyrazolones is described via the condensation of ninhydrin (indan‐1,2,3‐trione), phenylhydrazine, and various aldehydes in the presence of MMT@Fe3O4 as an environmentally benign core/shell nanocomposite catalyst. The catalyst could be recycled using an external magnet easily and reused several times without remarkable loss of its catalytic activity. Furthermore, avoiding hazardous solvents, reusability of the catalyst, easy work‐up, short reaction times, room temperature, and mild reaction conditions are the advantages of this new eco‐friendly protocol.

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Synthesis, biological evaluation and molecular modeling study of pyrazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents

Cited by 83 publications

References 51 publications

Crystal structure of N′-(4-(dimethylamino)benzylidene)-5-phenyl-1H-pyrazole-3-carbohydrazide, C₁₉H₁₉N₅O

Crystal structure of N′-(4-(dimethylamino)benzylidene)-5-phenyl-1H-pyrazole-3-carbohydrazide, C₁₉H₁₉N₅O

Synthesis of Fused Indolo‐Pyrazoles and Their Antimicrobial and Insecticidal Activities against Anopheles arabiensis Mosquito

The Novel Synthesis of Functionalized Indenopyrazolones Using Fe₃O₄ nanoparticles stabilized on MMT: An Efficient Magnetically Recoverable Heterogeneous Nanocomposite Catalyst

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Synthesis, biological evaluation and molecular modeling study of pyrazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents

Cited by 83 publications

References 51 publications

Crystal structure of N′-(4-(dimethylamino)benzylidene)-5-phenyl-1H-pyrazole-3-carbohydrazide, C19H19N5O

Crystal structure of N′-(4-(dimethylamino)benzylidene)-5-phenyl-1H-pyrazole-3-carbohydrazide, C19H19N5O

Synthesis of Fused Indolo‐Pyrazoles and Their Antimicrobial and Insecticidal Activities against Anopheles arabiensis Mosquito

The Novel Synthesis of Functionalized Indenopyrazolones Using Fe3O4 nanoparticles stabilized on MMT: An Efficient Magnetically Recoverable Heterogeneous Nanocomposite Catalyst

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Crystal structure of N′-(4-(dimethylamino)benzylidene)-5-phenyl-1H-pyrazole-3-carbohydrazide, C₁₉H₁₉N₅O

Crystal structure of N′-(4-(dimethylamino)benzylidene)-5-phenyl-1H-pyrazole-3-carbohydrazide, C₁₉H₁₉N₅O

The Novel Synthesis of Functionalized Indenopyrazolones Using Fe₃O₄ nanoparticles stabilized on MMT: An Efficient Magnetically Recoverable Heterogeneous Nanocomposite Catalyst