Screening and Evaluation of Antioxidant Activity of Some 1,2,4-triazolo[1,5-
            <i>a</i>
            ]quinazoline Derivatives

Al‐Salahi, Rashad; Anouar, El Hassane; Marzouk, Mohamed; Taie, Hanan A.A.; Abuelizz, Hatem A.

doi:10.4155/fmc-2017-0224

Cited by 36 publications

(40 citation statements)

References 38 publications

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“…In human system, a fine biological balance between the ordinary physiological production of ROS/RNS and their removal is already existed. However, an excess of oxidative stress can lead to the oxidation of biomolecules, which is accompanied with cell damage and embroil in the pathogenesis of many human diseases (Al-Salahi et al, 2017, Bak et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

Investigation the antioxidant activity of benzo[g]triazoloquinazolines correlated with a DFT study

Almehizia

Abuelizz

Taie

et al. 2019

Saudi Pharmaceutical Journal

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Previously, a series of 2-phenoxy-benzo[g]triazoloquinazolines 1–16 were synthesized and fully characterized. The antioxidant activity of the target molecules 1–16 was evaluated using three different assays namely 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging, ferric reduction antioxidant power (FRAP) and reducing power capability (RPC). The results revealed that some benzotriazoloquinazolines showed good activity and have the capacity to scavenge free radicals. In particular, compounds 1 and 14 have shown the highest activity. The butylated hydroxyl toluene (BHT) used as standard agent.Density functional theory was carried out to explain the relative importance of CO, CS and NH groups on the radical scavenging activity of the target benzotriazoloquinazolines. The finding in present study shows that the active compounds can be used as template for further development of more potent antioxidant agents.

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Section: Introductionmentioning

confidence: 99%

Investigation the antioxidant activity of benzo[g]triazoloquinazolines correlated with a DFT study

Almehizia

Abuelizz

Taie

et al. 2019

Saudi Pharmaceutical Journal

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“…In our previous paper [8,13], we have reported in detail the methodology routes for determination of DPPH radical scavenging activity %, FRAP values and reducing power of the target compounds.…”

Section: Antioxidant Assaysmentioning

confidence: 99%

“…The DPPH, FRAP and RPC assays were applied to assess the in vitro antioxidant activity of the pyrido-triazolopyrimidines (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17). The obtained results were presented in figures 1-3 and compared with standard synthetic antioxidant.…”

Section: Antioxidant Activitymentioning

confidence: 99%

“…Triazolo-annelated quinazolines were found to be potent adenosine antagonists, herbicidal and fungicidal agents [1][2][3]. In addition, further chemical transformation of their inherent lactam groups and substituent types at positions 2 and 5 were offered access to a variety of derivatives that have shown antihistamine, antimicrobial, antiviral, antihypertensive, anti-inflammatory, antitumor and antioxidant activities [4][5][6][7][8][9][10][11]. In light of the abovementioned facts, we are interested in the conversion of triazolquinazoline moiety into a pyridotriazolopyrimidine scaffold.…”

Section: Introductionmentioning

confidence: 99%

“…The emergence of various diseases resulting from oxidative stress such as diabetes, cancer, stroke, and cardiovascular dysfunctions, requires a permanent revaluation search and adjustment of adequate strategy to design and develop new bioactive substances to protect the human body against such diseases. In continuation of our on-going program research dealing with antioxidants, this research deals with the preparation and characterization of 2-methylthio-pyrido-triazolopyrimidines (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17); thereafter, evaluating their antioxidant activity using different assays.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and antioxidant activity of 2-methylthio-pyrido[3,2-e][1,2,4] triazolo[1,5-a]pyrimidines

et al. 2019

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A series of 2-methylthio-pyrido-triazolopyrimidines (1-17) were prepared by the reaction of dimethyl-N-cyanoimidodithiocarbonate with hydrazinopyridine carboxylic acid as starting reactants. Their chemical structures were affirmed with HREI-MS, IR and NMR analyses. The target compounds (1-17) were evaluated for their antioxidant activity using 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging, ferric reduction antioxidant power (FRAP) and reducing power capability (RPC). The results revealed that some pyrido-triazolopyrimidines showed good activity as antioxidant agents, in particular, compounds 12 and 15 were found to possess good antioxidant activity. Butylated hydroxyl toluene (BHT) was used as reference drug.

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PIFA Mediated Synthesis of Bis‐1,2,4‐triazoloquinazolines as Potential Anticancer Agents on MCF‐7 Cancer Cells: Characterization, Molecular Docking, Antiproliferative and ADME Profile

Kumar,

Bains,

Kamal

et al. 2023

ChemistrySelect

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A novel series of bis([1,2,4]triazolo)[4,3‐a][4′,3′‐c] quinazolines derivatives 2 a–2 o has been synthesis in good to excellent yields (74–86 %) under mild reaction conditions via bis(trifluoroacetoxy)iodobenzene (PIFA) mediated oxidative‐cyclization of corresponding 2,4‐bis(2‐(E)‐arylidenehydrazinyl) quinazolines 1 a–1 o. Formation of the targeted compounds has been supported using various spectroscopic tools (IR, 1H & 13 C‐NMR) and HRMS analysis. These bis([1,2,4]triazolo)[4,3‐a][4′,3′‐c] quinazolines derivatives were biologically screened for their antiproliferative activities against MCF‐7 cancer cells. Results indicate that among all synthesized derivatives, 3,7‐bis (4‐chlorophenyl) bis([1,2,4]triazolo)[4,3‐a : 4′,3′‐c]quinazoline (2 d) and 3,7‐bis(3‐methoxyphenyl)bis([1,2,4]triazolo)[4,3‐a : 4′,3′‐c]quinazoline (2 j) displayed uppermost cytotoxicity efficacy with GI50 value of 106.30 μM and 108.56 μM respectively. Furthermore, molecular docking studies have been carried out to investigate possible binding modes between active sites of the protein (PDB ID: 3 U6 J) and the target compounds. In addition to these results, ADME (adsorption, distribution, metabolism, excretion) analysis has also been carried out to study the pharmacokinetic properties of the targeted compounds.

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Screening and Evaluation of Antioxidant Activity of Some 1,2,4-triazolo[1,5- a ]quinazoline Derivatives

Abstract: Chemical modifications together with density functional theory study on the targets supplied us with some valuable clarifications about the required properties needed for the target compounds to be more active against free radicals.

Cited by 36 publications

References 38 publications

Investigation the antioxidant activity of benzo[g]triazoloquinazolines correlated with a DFT study

Investigation the antioxidant activity of benzo[g]triazoloquinazolines correlated with a DFT study

Synthesis and antioxidant activity of 2-methylthio-pyrido[3,2-e][1,2,4] triazolo[1,5-a]pyrimidines

PIFA Mediated Synthesis of Bis‐1,2,4‐triazoloquinazolines as Potential Anticancer Agents on MCF‐7 Cancer Cells: Characterization, Molecular Docking, Antiproliferative and ADME Profile

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