1-Acylthiosemicarbazides, 1,2,4-triazole-5(4H)-thiones, 1,3,4-thiadiazoles and hydrazones containing 5-methyl-2-benzoxazolinones: Synthesis, analgesic-anti-inflammatory and antimicrobial activities

Salgın-Gökşen, Umut; Gökhan-Kelekçi, Nesrin; Göktaş, Özgür; Köysal, Yavuz; Kılıç, Ekrem; Işık, Şamil; Aktay, Göknur; Özalp, Meral

doi:10.1016/j.bmc.2007.06.006

Cited by 331 publications

(146 citation statements)

References 38 publications

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“…6 Pharmacophoric hydrazone derivatives are newly designed based on highly bio-activity, appear vital activity and biologically important position. The interesting and valuable field for variety of heterocyclic compounds prepared from sulphur hydrazides, because they have medication active like antibacterial, 7 exhibit a great interest due to their importance in synthesis a which have antifungal, 8 antiinflammatory 9 herbicidal, 10 inhibitory activity, 11 analgesic activity, 12 anticholinergic and antihistaminic, 13 activity of regulating growth in plant 14 etc. Within the above view, no information available in literature in the past for synthesis and infectious activities of 2-benzylidene-1-tosylhydrazines.…”

Section: Introductionmentioning

confidence: 99%

Thionyl Chloride Catalyzed Synthesis and Antimicrobial Activities of Some 2-Benzylidene-1-Tosylhydrazines

Manikandan¹,

Balaji²,

Senbagam³

et al. 2017

ECB

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Section: Introductionmentioning

confidence: 99%

Thionyl Chloride Catalyzed Synthesis and Antimicrobial Activities of Some 2-Benzylidene-1-Tosylhydrazines

Manikandan¹,

Balaji²,

Senbagam³

et al. 2017

ECB

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“…It is well known that the hydrazone group provides a wide range of applications in biological and pharmaceutical fields. Therefore, a number of hydrazone derivatives have been claimed to possess interesting anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antitumoral and antiviral activities [12][13][14][15][16][17][18][19]. Furthermore, hydrazones can display antitubercular effects based on their tendency to form stable metal chelates with transition metal ions [20], which catalyze the physiological processes [21].…”

Section: Introductionmentioning

confidence: 99%

DETERMINATION OF THE DISSOCIATION CONSTANTS OF SOME p-SUBSTITUTED AROMATIC HYDRAZONES

Jankulovska¹,

Spirevska²,

Ragjenovikj³

2017

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A b s t r a c t: The acid-base behavior of five p-substituted aromatic hydrazones has been studied, using UV spectrophotometric method. The influence of the acidity of the medium on the absorption spectra is followed in aqueous sodium hydroxide solutions in pH region from 7 to 14. The measurements are performed at room temperature, and at ionic strength of 0.1, 0.25 and 0.5 mol dm -3 . A batochromic shift of the absorption band that appears in neutral media is observed, when pH is up to 7. It suggests that the dissociation process of the amide and hydroxyl group takes place. Deprotonation enthalpies and total energy values are calculated by using the semiempirical methods AM1 and PM3. Using the changes in the UV spectra with pH of the solution, the determination of dissociation constants, pK BH , at three different ionic strengths, as well as, the thermodynamic dissociation constants at zero ionic strength, is performed. In order to obtain more precise results, the calculations are made from the absorbance values at four selected wavelengths. Furthermore, the pK BH values were determined graphically from the intercept of the dependence of logI on pH. The results showed that the numerically calculated pK BH values are identical to those graphically obtained.

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“…1,2,4-Triazoles and their condensed derivatives have been investigated due to their wide range of bioactivities, including antimicrobial [5][6][7][8] , analgesic-anti-inflammatory [9] , antifungal [10] , herbicidal [11] , insecticidal activity [12] , anticancer [13,14] , and antigenotoxic activity [15] . It is known that the incorporation of a ferrocene fragment into a molecule of an organic compound often produces unexpected biological activity, likely due to different membrane permeation properties and anomalous metabolism.…”

Section: Introductionmentioning

confidence: 99%

Novel ferrocenyl derivatives exert anti-cancer effect in human lung cancer cells in vitro via inducing G1-phase arrest and senescence

Han

et al. 2013

Acta Pharmacol Sin

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Aim: To investigate the effects of 7 novel 1-ferrocenyl-2-(5-phenyl-1H-1,2,4-triazol-3-ylthio) ethanone derivatives on human lung cancer cells in vitro and to determine the mechanisms of action. Methods: A549 human lung cancer cells were examined. Cell viability was analyzed with MTT assay. Cell apoptosis and senescence were examined using Hoechst 33258 and senescence-associated-β-galactosidase (SA-β-gal) staining, respectively. LDH release was measured using a detection kit. Cell cycle was analyzed using a flow cytometer. Intracellular ROS level was measured with the 2′,7′-dichlorodihydrofluorescein probe. Phosphorylation of p38 was determined using Western blot. Results: Compounds 5b, 5d, and 5e (40 and 80 µmol/L) caused significant decrease of A549 cell viability, while other 4 compounds had no effect on the cells. Compounds 5b, 5d, and 5e (80 µmol/L) induced G 1 -phase arrest (increased the G 1 population by 22.6%, 24.23%, and 26.53%, respectively), and markedly increased SA-β-gal-positive cells. However, the compounds did not cause nuclear DNA frag mentation and chromatin condensation in A549 cells. Nor did they affect the release of LDH from the cells. The compounds significantly elevated the intracellular ROS level, decreased the mitochondrial membrane potential, and increased p38 phosphorylation in the cells. In the presence of the antioxidant and free radical scavenger N-acetyl-L-cysteine (10 mmol/L), above effects of compounds 5b, 5d, and 5e were abolished. Conclusion: The compounds 5b, 5d, and 5e cause neither apoptosis nor necrosis of A549 cells, but exert anti-cancer effect via inducing G 1 -phase arrest and senescence through ROS/p38 MAP-kinase pathway.

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1-Acylthiosemicarbazides, 1,2,4-triazole-5(4H)-thiones, 1,3,4-thiadiazoles and hydrazones containing 5-methyl-2-benzoxazolinones: Synthesis, analgesic-anti-inflammatory and antimicrobial activities

Cited by 331 publications

References 38 publications

Thionyl Chloride Catalyzed Synthesis and Antimicrobial Activities of Some 2-Benzylidene-1-Tosylhydrazines

Thionyl Chloride Catalyzed Synthesis and Antimicrobial Activities of Some 2-Benzylidene-1-Tosylhydrazines

DETERMINATION OF THE DISSOCIATION CONSTANTS OF SOME p-SUBSTITUTED AROMATIC HYDRAZONES

Novel ferrocenyl derivatives exert anti-cancer effect in human lung cancer cells in vitro via inducing G1-phase arrest and senescence

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