Synthesis, Characterization and Antioxidant Evaluation of Some Tetrazole Derivatives

Dalal, Meinaa Jaber; Mekky, Athraa Hameed

doi:10.22146/ijc.74912

Cited by 3 publications

(2 citation statements)

References 17 publications

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“…[3][4][5]. It has a wide use in medicinal chemistry as anti-hyperglycemic [4], antiinflammatory [5][6], antiviral [7][8], anticancer [9], antioxidants [10]. In this study, tetrazole was produced from cyclization of primary amine, sodium azide and triethyl orthoformate [11][12].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterization and Theoretical study of some 2-Oxopyridine Carbonitrile derivatives that contain tetrazole ring and evaluation of their Biological activity

Mekky,

Jaber Dalal,

G. Sager

et al. 2023

UTJsci

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A series of 2-oxo-6-[4-(1H-tetrazol-1-yl) phenyl-1,2-dihydropyridine-3-carbonitrile 3,4-dimethoxyphenyl)-2-oxo-6-4-(1H-tetrazol-1-yl) phenyl]-1,2-dihydropyridine-3-carbonitrile and 2-oxo-6-[4-(1H-tetrazol-1-yl) phenyl]-4-(thiophen-2-yl)- 1,2-dihydropyridine-3-carbonitrile), were prepared from the reaction of 4-aminoacetophenone, sodium azide in the presence of glacial acetic acid via cyclization reaction to produce (1-(4-(1H- 1,2,3,4tetrazole-1-yl) phenyl) ethan-1-one). Followed by condensation of (1-(4-(1H- 1,2,3,4tetrazole-1-yl) phenyl) ethan-1-one) with ethyl cyanoacetate, aromatic aldehydes, and ammonium acetate at 110℃ to give(3,4-dimethoxyphenyl)-2-oxo-6-4-(1H-tetrazol-1-yl)phenyl]-1,2-dihydropyridine-3-carbonitrile and 2-oxo-6-[4-(1H-tetrazol-1-yl) phenyl-1,2-dihydropyridine-3-carbonitrile 3,4-dimethoxyphenyl)-2-oxo-6-4-(1H-tetrazol-1-yl) phenyl]-1,2-dihydropyridine-3-carbonitrile and 2-oxo-6-[4-(1H-tetrazol-1-yl) phenyl]-4-(thiophen-2-yl)- 1,2-dihydropyridine-3-carbonitrile. The synthesized compounds were characterized by spectral methods (FT-IR and 1H-NMR & 13C-NMR). The synthesized compounds have been estimated in lab. for biological efficiency. Preliminary biological testing reveals that the compounds have exhibited activity against the two types of bacteria (staphylococcus aureus, and Klebsiella pneumonia). Both Compounds had high activities. Docking experiments for the compounds were undertaken in order to better understand the ligand-protein interactions in terms were done using py-px and BIOVIA/ Discovery studio of binding affinity. The computed binding affinities were consistent with the MIC values

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Section: Introductionmentioning

confidence: 99%

Synthesis, characterization and Theoretical study of some 2-Oxopyridine Carbonitrile derivatives that contain tetrazole ring and evaluation of their Biological activity

Mekky,

Jaber Dalal,

G. Sager

et al. 2023

UTJsci

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“…This tetrazole is used in an MTT assay to quantify the respiratory activity of live cells in cell culture, although it kills cells in the process 6 . Tetrazole derivatives have potential pharmacological activities such as antihypertensive 7 , antimicrobial 8 , corrosion inhibitor 9 , anti-inflammatory 10 , anticancer 11 , antioxidant 12 , analgesic 13 , antiviral 14 , protein arginine deiminase inhibitor 15 , anti-allergic 16 , dual selective serotonin and norepinephrine reuptake inhibitors 17 and HIV inhibitors 18 . They are used as catalysts in the synthesis of phosphonates.…”

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confidence: 99%

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2023

IJPSR

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A series of flavones derivatives 11(a-j) have been synthesized and evaluated for their in-vitro antibacterial and antifungal activities. The antibacterial screening data showed that compounds with 4-methoxyphenyl (11c), 4-fluorophenyl (11d), and 2, 5fluorophenyl (11h) substituent's on tetrazole ring, showed the maximum activity against the organisms used. The antifungal screening revealed that a compound with 4-nitropheny (11g) on tetrazole ring exhibited the highest activity against A. niger and a compound with 4-methoxyphenyl (11c) group exhibited good activity against C. albicans. INTRODUCTION:Flavones and their derivatives were considered potent antitumor activity, associated with their ability to induce apoptosis 1 . The drugs baicalein, 3, 7-dihydroxyflavone and chrysin, considered antitumor agents, act as inducers of apoptosis in tumor cells through caspases-dependent pathways 2 . The introduction of prenyl side chains on flavones increases in growth inhibitory activities towards tumor cell lines 3 , due to the effect related to the activation of caspase for some of the prenylated derivatives 4 . The alkylation/heteroarylation on flavones improved the antitumor activity 5 . Similarly, tetrazole and its derivatives can act as a pharmacophore for the carboxylate group, increasing their utility. Angiotensin II blocker often contain tetrazoles as Losartan and candesartan.

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Synthesis, Evaluation of anticancer and antimicrobial activities of some Schiff bases derivatives

Farhan,

Ibrahim,

Ali

2023

Al-Kitab J. Pure Sci.

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In this research, compound [1,2-Bis-(4-amino-5-mercapto-4H-[1,2,4]triazol-3-yl)-ethane-1,2-diol] was used as starting material for synthesis different Schiff's Bases compounds. The fusion of tartaric acid with thiocarbohydrazide produce the compound (C1), the Schiff's bases (C2-C4) were created through the condensation of substances (C1) with different substituted benzaldehydes in presence of glacial acetic acid as catalyst. Thin layer chromatography (TLC) was used to confirm the compounds' purity, and spectroscopic methods were used to infer the compounds' structures (FTIR) and magnetic nuclear resonance spectroscopy (1H-NMR and 13C-NMR). The agar well diffusion method was used to test synthesized compounds for their antibacterial activity against K. pneumonia and S. aureus, and the findings were inconsistent. Target substances were tested for their ability to kill human breast cancer at concentrations of 50 and 100 g/mL. Human muscle tissue HC normal cell line, human cervical cancer Hela cell line, and HePG2 cell line. The results showed that the chemicals had potential cytotoxic activity against the Hela cell line, particularly compound (C4), which had the greatest inhibition at doses of 100 mg/mL among the examined substances

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Synthesis, Characterization and Antioxidant Evaluation of Some Tetrazole Derivatives

Cited by 3 publications

References 17 publications

Synthesis, characterization and Theoretical study of some 2-Oxopyridine Carbonitrile derivatives that contain tetrazole ring and evaluation of their Biological activity

Synthesis, characterization and Theoretical study of some 2-Oxopyridine Carbonitrile derivatives that contain tetrazole ring and evaluation of their Biological activity

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Synthesis, Evaluation of anticancer and antimicrobial activities of some Schiff bases derivatives

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