Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents

Amir, Mohd; Kumar, Harish; Khan, Shahrukh Rafi

doi:10.1016/j.bmcl.2007.12.043

Cited by 233 publications

(120 citation statements)

References 19 publications

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“…Due to their topology and nature of donor atoms, pyrazole derivatives have drawn great interest in agrochemical, pharmaceutical, and chemical industries [2,3]. Nitrogen containing five membered heterocyclic compounds could be used as antitumor, antibacterial, antifungal, antiviral, anti-parasitic, anti-tubercular and insecticidal agents [4,5]. They have been studied extensively for useful biological effectiveness such as anti-inflammatory, anti-diabetic, anesthetic and analgesic properties [6,7].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Crystal Structure of Bis[1-methoxy-2,2,2-tris-(pyrazol-1-yl-κN2)ethane]-copper(II) Bis-perchlorate

Lyubartseva¹,

Parkin²,

Ngongoni³

et al. 2016

JCCE

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Bis[1-methoxy-2,2,2-tris-(pyrazol-1-yl-κN 2 )ethane]-copper(II) bis-perchlorate (2) was synthesized by reacting of pyrazole based tripodal scorpionate ligand 1-methoxy-2,2,2-tris(pyrazol-1-yl)ethane (1) with copper(II) perchlorate hexahydrate in methanol, acetonitrile and water mixture as solvent. Slow evaporation of the filtered reaction mixture in air produced blue color block crystals suitable for single crystal X-ray diffraction study of the title complex. Compound 2 crystallizes in the monoclinic space group P2 1 /n with unit cell parameters, a = 8.1269(1) Ả, b = 21.8348(2)Ả, c = 9.1522(1) Å, α = γ = 90º, β = 99.7611(4)º. The structure of the compound was characterized by IR Spectroscopy, elemental analysis and single crystal X-ray diffraction analysis.

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Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Crystal Structure of Bis[1-methoxy-2,2,2-tris-(pyrazol-1-yl-κN2)ethane]-copper(II) Bis-perchlorate

Lyubartseva¹,

Parkin²,

Ngongoni³

et al. 2016

JCCE

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“…Many pyrazole derivatives are reported to have a broad spectrum of biological activities, such as anti-inflammatory [13], antifungal [14], antiviral [15], cytotoxic [12], A3 adenosine receptor antagonists [16], antioxidant [13], antihypertensive [17], tranquilizing, muscle relaxant, psychoanaleptic, hypnotic, ulcerogenic, antidepressant, antibacterial and analgesic effects [18]. Pharmacologically-interesting heterocyclic systems like pyrazolines have been widely studied owing to their pharmacological activities, which include anti-tumor [19,20], anti-inflammatory [21][22][23][24][25][26][27][28][29][30][31][32], anti-parasitary [33], anticonvulsant [34], antimicrobial [35][36][37][38][39], antinociceptives [40], antimalarial [41], nitric oxide synthase inhibitory, associated with diseases such as Alzheimer, Huntington, and inflammatory arthritis [42], antidepressant [43,44], anticancer [45][46][47], antibacterial [48], antitubercular, analgesic [49], antiviral [46], antioxidant [50], antiamoebic …”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antibacterial and Antifungal Activity of Some New Pyrazoline and Pyrazole Derivatives

Hassan

2013

Molecules

142

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A series of 2-pyrazolines 5-9 have been synthesized from α,β-unsaturated ketones 2-4. New 2-pyrazoline derivatives 13-15 bearing benzenesulfonamide moieties were then synthesized by condensing the appropriate chalcones 2-4 with 4-hydrazinyl benzenesulfonamide hydrochloride. Ethyl [1,2,4] Condensation of 6,6-dimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indole-2-carbaldehyde (1') with compound 24 or 25 afforded the corresponding Schiff's bases 36 and 37, respectively. Reaction of the Schiff's base 37 with benzoyl hydrazine or acetic anhydride afforded benzohydrazide derivative 39 and the cyclized compound 40, respectively. Furthermore, the pyrazole derivatives 42-44 were synthesized by cyclization of hydrazine derivative 25 with the prepared chalcones 2-4. All the newly synthesized compounds have been characterized on the basis of IR and 1 H-NMR spectral data as well as physical data.Antimicrobial activity against the organisms E. coli ATCC8739 and P. aeruginosa ATCC 9027 as examples of Gram-negative bacteria, S. aureus ATCC 6583P as an example of Gram-positive bacteria and C. albicans ATCC 2091 as an example of a yeast-like fungus have been studied using the Nutrient Agar (NA) and Sabouraud Dextrose Agar (SDA) diffusion methods. The best performance was found for the compounds 16, 17, 19 and 20.

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“…Pyrazoline compounds are acquiring more importance because of their immense biological and pharmacological potential. This class of compound possesses wide spectrum of biological activities such as antimicrobial [1,2,3], anti-inflammatory and analgesic [4,5], anticancer [6,7], antidepressant [8], anti-tuberculosis [9,10], antiamoebic [11] antioxidant [12,13], antihyperglycemic [14], anti-epileptic [15,16], anti-parkinson and anti-alzheimer [17].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Activity of Novel Series of Diversely Substituted Acetyl Pyrazoline Bearing Biphenyl Carbonitrile Motif

Patel

Karia

2016

ILCPA

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Abstract. Novel series of diversely substituted acetyl pyrazoline having biphenyl carbonitrile motif have been synthesized. The reaction of 2-cyno-4'-bromomethyl biphenyl with1-(4-hydroxyphenyl)-ethanone resulted in acetophenone derivative of biphenyl-2-carbonitrile. This acetophenone derivative was condensed with substituted aromatic aldehyde in mixed solvent resulted in various substituted chalcones. These chalcones were further cyclized using hydrazine hydrate in presence of glacial acetic acid to produce titled compound derivatives. The chemical structures of synthesized compounds were elucidated by 1 H-NMR, 13C-NMR FT-IR and mass spectra. Synthesized compounds were screened for their antimicrobial activity by broth dilution method. Out of twelve newly synthesized compounds, eight compounds are found to be equipotent to Ampicillin. Introduction:

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Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents

Cited by 233 publications

References 19 publications

Synthesis, Characterization and Crystal Structure of Bis[1-methoxy-2,2,2-tris-(pyrazol-1-yl-κN2)ethane]-copper(II) Bis-perchlorate

Synthesis, Characterization and Crystal Structure of Bis[1-methoxy-2,2,2-tris-(pyrazol-1-yl-κN2)ethane]-copper(II) Bis-perchlorate

Synthesis, Antibacterial and Antifungal Activity of Some New Pyrazoline and Pyrazole Derivatives

Synthesis and Antimicrobial Activity of Novel Series of Diversely Substituted Acetyl Pyrazoline Bearing Biphenyl Carbonitrile Motif

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