Molecular salts of terephthalic acids with 2-aminopyridine and 2-aminothiazole derivatives as potential antioxidant agents; Base-Acid-Base type architectures

Khan, Ezzat; Khan, Abdullah; Gul, Zarif; Ullah, Farhat; Tahir, Muhammad Nawaz; Khalid, Muhammad; Asif, Hafiz Muhammad; Asim, Sumreen; Braga, Ataualpa Albert Carmo

doi:10.1016/j.molstruc.2019.127126

Cited by 27 publications

(17 citation statements)

References 55 publications

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“…Anticholinesterase activity of compounds 1-6 was evaluated by Ellman's assay using two enzymes, AChE and BChE and following our previously reported protocol without further modifications [49][50][51]. The enzyme AChE is derived from Electric eel and BChE from equine serum [52].…”

Section: Anticholinesterase Evaluationmentioning

confidence: 99%

“…Absorbance of the incubated sample was measured at 412 nm by a double-beam spectrophotometer (Thermo Electron Corporation, USA) for 4 min along with the reaction time at 30 • C. The well-established Galanthamine was used as positive control and all experiments were performed in triplicate. The percent enzyme activity and enzyme inhibition by control and test samples were calculated from the rate of absorption with respect to change in time (V = ∆Abs/∆t) using the same procedure as reported previously [49][50][51].…”

Section: Anticholinesterase Evaluationmentioning

confidence: 99%

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Thiourea Derivatives, Simple in Structure but Efficient Enzyme Inhibitors and Mercury Sensors

et al. 2021

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In this study six unsymmetrical thiourea derivatives, 1-isobutyl-3-cyclohexylthiourea (1), 1-tert-butyl-3-cyclohexylthiourea (2), 1-(3-chlorophenyl)-3-cyclohexylthiourea (3), 1-(1,1-dibutyl)-3-phenylthiourea (4), 1-(2-chlorophenyl)-3-phenylthiourea (5) and 1-(4-chlorophenyl)-3-phenylthiourea (6) were obtained in the laboratory under aerobic conditions. Compounds 3 and 4 are crystalline and their structure was determined for their single crystal. Compounds 3 is monoclinic system with space group P21/n while compound 4 is trigonal, space group R3:H. Compounds (1–6) were tested for their anti-cholinesterase activity against acetylcholinesterase and butyrylcholinesterase (hereafter abbreviated as, AChE and BChE, respectively). Potentials (all compounds) as sensing probes for determination of deadly toxic metal (mercury) using spectrofluorimetric technique were also investigated. Compound 3 exhibited better enzyme inhibition IC50 values of 50, and 60 µg/mL against AChE and BChE with docking score of −10.01, and −8.04 kJ/mol, respectively. The compound also showed moderate sensitivity during fluorescence studies.

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Section: Anticholinesterase Evaluationmentioning

confidence: 99%

Section: Anticholinesterase Evaluationmentioning

confidence: 99%

Thiourea Derivatives, Simple in Structure but Efficient Enzyme Inhibitors and Mercury Sensors

et al. 2021

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“…Prior to the determination of absorbance, all solutions were incubated in the dark for 30 min at room temperature (23 ± 1 • C). The percent inhibition capacity of each complex (I)%, was calculated as below [36].…”

Section: Determination Of Antioxidant Potentialsmentioning

confidence: 99%

Complexes of 1,3-Diisobutyl Thiourea with Copper(I), Zinc(II) and Mercury(II): Their Antioxidant and Antibacterial Evaluation

et al. 2021

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The reaction of 1,3-Diisobutyl thiourea (Tu) with metal salts, {[CuX (X = Cl, I)], [ZnCl2] and [HgI2] in an appropriate stoichiometric ratio afforded the corresponding metal complexes [Tu2CuCl] (1), [Tu3CuI] (2), [Tu2ZnCl2] (3) and [Tu2HgI2] (4) in good yields. The FT-IR data show typically broad signals (3278–3288 cm−1) attributed to the involvement of NH bonds in extensive hydrogen bonding. The structures of complexes were proposed based on a spectroscopic data set. Compounds 1 and 2 were additionally characterized by single-crystal X-ray analysis. Complexes 1–4 were tested for their free radical scavenging efficiency using 2,2-diphenyl-1-picrylhydrazyl free radical (hereafter abbreviated as DPPH). The free radical scavenging activity was a function of decrease in the resultant absorption of DPPH solution after the mixing of an appropriate concentration of the respective complex. The activity of complexes was determined to be dose dependent and increased concentration of the complex resulted in improved antioxidant activity. Compound 1 was found to be the most efficient, with 79.9% free radical scavenging activity. Complexes were also tested for their efficiency against selected strains of bacteria (E. coli, S. flexneri, S. typhi, and P. aeruginosa) and the activities were compared to commercially available standard drug cephradine. Compound 1 was more active against P.aeruginosa (ZI 13.25), while compound 4 was found to be more active against E. coli (ZI 11.0), S. flexneri (ZI 11.2), and S. typhi (ZI 10.5).

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“…There are many substituted thiazole-containing heterocycles covering a wide range of therapeutic targets including antimicrobial, anticancer, anti-inflammatory and anti-HIV. Aminothiazole scaffolds are important structural units in medicinal chemistry as they have shown antitumor [ 1 , 2 , 3 ], antiviral [ 4 , 5 , 6 ], antibacterial [ 7 , 8 , 9 ], anti-prion [ 10 ], psychotropic [ 11 ], anti-allergic [ 12 ], anti-hypertensive [ 13 ], anti-inflammatory [ 14 , 15 ], antifungal [ 16 ], antitubercular [ 17 , 18 ], anti-HIV [ 19 ], pesticidal [ 20 ], antiprotozoal [ 21 ], antipyretic [ 22 ], antioxidative [ 23 ] and analgesic activities [ 24 ]. Aminothiazole compounds act as ligands of estrogen receptors [ 25 ] and afford a new group of adenosine receptor antagonists [ 26 ].…”

Section: Introductionmentioning

confidence: 99%

An Overview on Synthetic 2-Aminothiazole-Based Compounds Associated with Four Biological Activities

2021

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Amongst sulfur- and nitrogen-containing heterocyclic compounds, the 2-aminothiazole scaffold is one of the characteristic structures in drug development as this essential revelation has several biological activities abiding it to act as an anticancer, antioxidant, antimicrobial and anti-inflammatory agent, among other things. Additionally, various 2-aminothiazole-based derivatives as medical drugs have been broadly used to remedy different kinds of diseases with high therapeutic influence, which has led to their wide innovations. Owing to their wide scale of biological activities, their structural variations have produced attention amongst medicinal chemists. The present review highlights the recently synthesized 2-aminothiazole-containing compounds in the last thirteen years (2008–2020). The originality of this proposal is based on the synthetic strategies developed to access the novel 2-aminothiazole derivatives (N-substituted, 3-substituted, 4-substituted, multi-substituted, aryl/alkyl substituents or acyl/other substituents). The literature reports many synthetic pathways of these 2-aminothiazoles associated with four different biological activities (anticancer, antioxidant, antimicrobial and anti-inflammatory activities). It is wished that this review will be accommodating for new views in the expedition for rationalistic designs of 2-aminothiazole-based medical synthetic pathways.

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Molecular salts of terephthalic acids with 2-aminopyridine and 2-aminothiazole derivatives as potential antioxidant agents; Base-Acid-Base type architectures

Cited by 27 publications

References 55 publications

Thiourea Derivatives, Simple in Structure but Efficient Enzyme Inhibitors and Mercury Sensors

Thiourea Derivatives, Simple in Structure but Efficient Enzyme Inhibitors and Mercury Sensors

Complexes of 1,3-Diisobutyl Thiourea with Copper(I), Zinc(II) and Mercury(II): Their Antioxidant and Antibacterial Evaluation

An Overview on Synthetic 2-Aminothiazole-Based Compounds Associated with Four Biological Activities

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