Design, synthesis and pharmacological evaluation of some novel derivatives of 1-{[3-(furan-2-yl)-5-phenyl-4,5-dihydro-1,2-oxazol-4-yl]methyl}-4-methyl piperazine

Kumar, J. Kranthi; Chawla, Gita; Akhtar, Mohd; Sahu, Kapendra; Rathore, Vandana; Sahu, Shikha

doi:10.1016/j.arabjc.2013.04.027

Cited by 20 publications

(13 citation statements)

References 22 publications

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“…The propen‐1‐one derivatives ( 11a–l ) were prepared via base catalyzed condensation of the appropriate aromatic aldehyde and the corresponding ketone in methanol using reported procedures . Cyclocondensation of the appropriate chalcone ( 11a–l ) with 4‐methanesulfonylphenylhydrazinehydrochloride ( 12 ) in aqueous ethanol afforded the respective triarylpyrazolines ( 13a–l ) as racemic mixtures in good yields (62–88%) (Scheme ).…”

Section: Resultsmentioning

confidence: 99%

Synthesis, Cyclooxygenase Inhibition, Anti‐Inflammatory Evaluation, and Ulcerogenic Liability of New 1,3,5‐Triarylpyrazoline Derivatives Possessing a Methanesulfonyl Pharmacophore

Abdellatif

Fadaly

Azouz

2016

Archiv der Pharmazie

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A new series of 1,3,5-triarylpyrazolines 13a-l was synthesized and all prepared compounds were evaluated for their in vitro COX-1/COX-2 inhibitory activity and in vivo anti-inflammatory activity. All test compounds were more selective for the COX-2 isozyme and showed good in vivo anti-inflammatory activity. Compound 13h was the most COX-2 selective compound (COX-2 selectivity index (SI) = 10.23) and the most potent anti-inflammatory derivative (ED = 60.1 µmol/kg) in comparison with celecoxib (COX-2 SI = 9.29 and ED = 81.4 µmol/kg). All screened compounds were less ulcerogenic (ulcer indexes (UI) = 0.33-1.33) than aspirin (UI = 2.33) and comparable to celecoxib (UI = 0.33).

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Section: Resultsmentioning

confidence: 99%

Synthesis, Cyclooxygenase Inhibition, Anti‐Inflammatory Evaluation, and Ulcerogenic Liability of New 1,3,5‐Triarylpyrazoline Derivatives Possessing a Methanesulfonyl Pharmacophore

Abdellatif

Fadaly

Azouz

2016

Archiv der Pharmazie

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“…Compounds 181a and 181b were reported as the most promising anxiolytics [289]. Amongst the compounds developed by Kumar et al, compounds 182a and 182b displayed considerable antianxiety activity [290].…”

Section: Anxiolytic Activitymentioning

confidence: 99%

Piperazine scaffold: A remarkable tool in generation of diverse pharmacological agents

Shaquiquzzaman

Verma

Marella

et al. 2015

European Journal of Medicinal Chemistry

198

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“…Evaluation of these compounds in cell lines expressing nicotinic receptor subtypes showed that the compounds had up to 10-fold higher affinity for α4β2 receptor than α3β2 receptor subtype. Kumar et al (2017) synthesized a series of 3,4,5-trisubstituted isoxazoles incorporating furan and piperazine moiety and evaluated for their antidepressant activity by Porsolt's forced swimming test on albino mice and antianxiety activity by plus maze method. Compounds 87a and 87b (Fig.…”

Section: Antidepressant Activitymentioning

confidence: 99%

The synthetic and therapeutic expedition of isoxazole and its analogs

2018

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Isoxazole, constituting an important family of five-membered heterocycles with one oxygen atom and one nitrogen atom at adjacent positions is of immense importance because of its wide spectrum of biological activities and therapeutic potential. It is, therefore, of prime importance that the development of new synthetic strategies and designing of new isoxazole derivatives should be based on the most recent knowledge emerging from the latest research. This review is an endeavor to highlight the progress in the chemistry and biological activity of isoxazole derivatives which could provide a low-height flying bird's eye view of isoxazole derivatives to the medicinal chemists for the development of clinically viable drugs using this information.

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Design, synthesis and pharmacological evaluation of some novel derivatives of 1-{[3-(furan-2-yl)-5-phenyl-4,5-dihydro-1,2-oxazol-4-yl]methyl}-4-methyl piperazine

Cited by 20 publications

References 22 publications

Synthesis, Cyclooxygenase Inhibition, Anti‐Inflammatory Evaluation, and Ulcerogenic Liability of New 1,3,5‐Triarylpyrazoline Derivatives Possessing a Methanesulfonyl Pharmacophore

Synthesis, Cyclooxygenase Inhibition, Anti‐Inflammatory Evaluation, and Ulcerogenic Liability of New 1,3,5‐Triarylpyrazoline Derivatives Possessing a Methanesulfonyl Pharmacophore

Piperazine scaffold: A remarkable tool in generation of diverse pharmacological agents

The synthetic and therapeutic expedition of isoxazole and its analogs

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