Synthesis and Antioxidant Activity of Some New Thiazolyl–Pyrazolone Derivatives

Gaffer, Hatem E.; Abdel-Fattah, Sherif A.; Etman, H. A.; Abdel‐Latif, Ehab

doi:10.1002/jhet.2588

Cited by 32 publications

(19 citation statements)

References 21 publications

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“…Gaffer and co-workers [106] screened the antioxidant activity of a cluster of thiazolyl-pyrazolone derivatives through 2, 2 0 -azinobis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical cation decolorization assay. Compounds 149 and 150 ( Fig.…”

Section: Antioxidant Agentsmentioning

confidence: 99%

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Zhao

Dai

et al. 2020

European Journal of Medicinal Chemistry

139

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a b s t r a c tThe pyrazolone structural motif is a critical element of drugs aimed at different biological end-points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates with several medicinal features including antimicrobial, antitumor, CNS (central nervous system) effect, anti-inflammatory activities and so on. Meanwhile, SAR (Structure-Activity Relationship) investigations have drawn attentions among medicinal chemists, along with a plenty of analogues have been derived for multiple targets. In this review, we comprehensively summarize the biological activity and SAR for pyrazolone analogues, wishing to give an overall retrospect and prospect on the pyrazolone derivatives.

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Section: Antioxidant Agentsmentioning

confidence: 99%

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Zhao

Dai

et al. 2020

European Journal of Medicinal Chemistry

139

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“…The antioxidant properties (Table ) of the synthesized nicotinonitrile‐based compounds were screened by using the 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulphonic acid) (ABTS) radical cation decolorization assay . The results indicated that clubbing between the nicotinonitrile moiety and thiazole ring in compounds 6a‐c promoted the antioxidant activity to the highest percent inhibition ranged from 82.15% to 86.27%.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and antioxidant assay of new nicotinonitrile analogues clubbed thiazole, pyrazole and/or pyridine ring systems

Abumelha

2020

Journal of Heterocyclic Chem

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A series of novel nicotinonitrile derivatives were synthesized by hybridization with thiazole, pyrazole, and pyridine ring systems using 4‐aminobenzohydrazide as link‐bridge. The synthetic strategy of nicotinonitrile‐thiazole analogues involves cyclization of the precursor N‐phenyl thiosemicarbazide derivative 4 with chloroacetic acid and phenacyl bromide. The reaction of hydrazide 3 with acetylacetone and/or ethyl acetoacetate was applied as a synthetic route for accessing 2‐((4‐(pyrazole‐1‐carbonyl)phenyl)amino)‐nicotinonitrile derivatives 9–10. The 2‐((4‐(4‐thiazolylidene‐pyrazole‐1‐carbonyl)‐phenyl)amino)nicotinonitriles 14–15 were obtained via a nucleophilic addition of pyrazolone 10 to phenyl isothiocyanate followed by cyclization with chloroacetone, phenacyl chloride, and/or ethyl bromoacetate. The 6‐amino‐4‐aryl‐3,5‐dicyano‐2‐oxo‐1‐(4‐substitutedbenzamido)‐pyridines 19 were synthesized by Knoevenagel condensation N′‐(2‐cyanoacetyl)‐benzohydrazide derivative 16 with substituted benzaldehydes followed by heating with malononitrile. All synthesized products were evaluated for their antioxidant potentialities using of 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulphonic acid) (ABTS) radical cation delcolorization assay. The nicotinonitrile‐thiazole hybrid 6b was found the most promising antioxidant agent with inhibition activity 86.27%.

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“…Wherever, the π‐electrons are delocalized afterward loss of the proton and the resulted antioxidant values for these derivative have been evaluated. Meanwhile, their reactivity correlates to the substituents type on the ring, and their concentrations to stand on their efficacy and structural activity relationship for these preps derivatives . Moreover, thiazolidinone analogues have a remarkable biological efficacies, such as antioxidant, antitumor, and also antimicrobial activity .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Pyrazolin‐5‐one Derivatives Clubbed with Thiazole and/or Thiadiazole and Evaluation of Their Antioxidant and Cytotoxic Activities

et al. 2019

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Synthesis of some new thiazolyl 2‐pyrazolin‐5‐one analogues was succeeded through the reaction of 3‐methyl‐1‐thiocarbamoyl‐2‐pyrazolin‐5‐one with different α‐halogenated derivatives via different routes. The physical and spectral analysis techniques were performed to demonstrate the proper structures of all incorporated analogues. The synthesized derivatives were investigated as cytotoxic agents against some important cell lines, in which the results displayed persuasive activities relative to the results of antibiotic standards. In addition, the antioxidant activity of the synthesized analogues was evaluated using ABTS•+ method. The preps analogues displayed respectable results as antioxidant agents, especially derivatives 14 a‐c and 11 a‐c due to the existence of thiadiazolyl and bis‐thaizolyl arms for pyrazoline ring, respectively.

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Synthesis and Antioxidant Activity of Some New Thiazolyl–Pyrazolone Derivatives

Cited by 32 publications

References 21 publications

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Synthesis and antioxidant assay of new nicotinonitrile analogues clubbed thiazole, pyrazole and/or pyridine ring systems

Synthesis of Pyrazolin‐5‐one Derivatives Clubbed with Thiazole and/or Thiadiazole and Evaluation of Their Antioxidant and Cytotoxic Activities

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