Synthesis, characterization and antimicrobial evaluation of ethyl 2-arylhydrazono-3-oxobutyrates

Küçükgüzel, Ş. Güniz; Rollas, Sevım; Erdeniz, Habibe; Kiraz, Mehmet Sabır

doi:10.1016/s0223-5234(99)80048-8

Cited by 59 publications

(21 citation statements)

References 11 publications

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“…Compound 17d showed significant activity against S. aureus whereas the others had no remarkable activity on this strain. Compound 17e was found to be more active than the others against Mycobacterium fortuitum at a MIC value of 32 μg/ml [31]. …”

Section: Antimicrobial Activitymentioning

confidence: 92%

Biological Activities of Hydrazone Derivatives

2007

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There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and antischistosomiasis activities. Hydrazones possessing an azometine -NHN=CH-proton constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observations have been guiding for the development of new hydrazones that possess varied biological activities.

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Section: Antimicrobial Activitymentioning

confidence: 92%

Biological Activities of Hydrazone Derivatives

2007

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“…This includes the formation of 1,3,4-thiadiazole derivatives in acidic media. The same thiosemicarbazides, in the presence of NaOH, underwent cyclisation to yield 1,2,4-triazole thione derivatives [14][15][16].…”

Section: Introductionmentioning

confidence: 99%

New Thiosemicarbazides and 1,2,4-Triazolethiones Derived from 2-(Ethylsulfanyl) Benzohydrazide as Potent Antioxidants

et al. 2014

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New thiosemicarbazide derivatives 2-6 were synthesised by reacting 2-(ethylsulfanyl)benzohydrazide with various aryl isothiocyanates. The cyclisation of compounds 2-6 under reflux conditions in a basic medium (aqueous NaOH, 4 N) yielded compounds 7-11 that contain a 1,2,4-triazole ring. All of the synthesised compounds were screened for their antioxidant activities. Compounds 2, 3, and 7 showed better radical scavenging in a 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, with IC 50 values of 1.08, 0.22, and 0.74 µg/mL, respectively, compared to gallic acid (IC 50 , 1.2 µg/mL). Compound 3 also showed superior results in a ferric reducing antioxidant power (FRAP) assay (3054 µM/100 g) compared to those of ascorbic acid (1207 µM/100 g).

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“…In addition, the fragmentation pattern for all compounds was supported in the mass spectra. 24,29 . IR, 1 H-NMR, 13 C-NMR and mass spectral data are in agreement with the proposed structures of all newly synthesized compounds.…”

Section: à124mentioning

confidence: 99%

Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles

Çıkla-Süzgün

Kaushik‐Basu

Basu

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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Arachidonic acid is an unsaturated fatty acid liberated from phospholipids of cell membranes. NSAIDs are known as targets of cyclooxygenase enzyme (COX-1, COX-2 and COX-3) in arachidonic acid metabolism. This mechanism of COX-2 in carcinogenesis causes cancer. In addition, COX-2 plays a role in the early stages of hepatocarcinogenesis. Hepatitis C virus (HCV) infection is cause of liver cirrhosis and hepatocellular carcinoma (HCC). The aim of our study was to improve effective agents against HCV. A novel series of new etodolac 1,2,4-triazoles derivatives (4a-h) have been synthesized and investigated for their activity against HCV NS5B polymerase. Compound 4a was found to be the most active with IC 50 value of 14.8 mM. In accordance with these results, compound 4a was screened for anti-cancer activity on liver cancer cell lines (Huh7, Mahlavu, HepG2, FOCUS). Compound 4a showed anti-cancer activity against Huh7 human hepatoma cell line with IC 50 value of 4.29 mM. Therefore, compound 4a could be considered as a new anti-cancer and anti-HCV lead compound.

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Synthesis, characterization and antimicrobial evaluation of ethyl 2-arylhydrazono-3-oxobutyrates

Cited by 59 publications

References 11 publications

Biological Activities of Hydrazone Derivatives

Biological Activities of Hydrazone Derivatives

New Thiosemicarbazides and 1,2,4-Triazolethiones Derived from 2-(Ethylsulfanyl) Benzohydrazide as Potent Antioxidants

Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles

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