Synthesis of some novel thiourea derivatives obtained from 5-[(4-aminophenoxy)methyl]-4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones and evaluation as antiviral/anti-HIV and anti-tuberculosis agents

Küçükgüzel, İlkay; Tatar, Esra; Küçükgüzel, Ş. Güniz; Rollas, Sevım; Clercq, Erik De

doi:10.1016/j.ejmech.2007.04.010

Cited by 193 publications

(82 citation statements)

References 44 publications

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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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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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“…It is foreseeable that more and more types of hydrazides including cyclic ones will be continuously served as reactants to prepare novel triazole derivatives with special properties, and the related researches will become increasingly active in future [157][158][159][160].…”

Section: Thiol Thio Hydrazidesmentioning

confidence: 99%

Current Developments in the Syntheses of 1,2,4-Triazole Compounds

Zhang¹,

Damu²,

Cai³

et al. 2014

COC

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Heterocyclic 1,2,4-triazole derivatives possess unusually spacious potentiality as medicinal agents, agricultural chemicals, functional materials, ionic liquids, supramolecular catalysts as well as artificial enzymes and receptors for supramolecular recognition and biomimetic catalysis, and their various researches and developments have been being a quite rapidly developing and active highlight topic with an infinite space. Numerous efforts have been directed toward various types of possible applications of 1,2,4-triazole-based compounds and a lot of important progress has been made, especially their preparations have attracted increasing attention. This review systematically summarized the recent advances in the syntheses of 1,2,4-triazole derivatives, including: (1) Cyclizations to form triazole ring; (2) Transformations of heterocyclic compounds to construct triazole ring; (3) Substitutions on 1,2,4-triazole ring; (4) Structural modifications in side chains of 1,2,4-triazole ring. It was hoped that this review would be helpful for the design and development of highly efficient preparation of 1,2,4-triazole derivatives with various sorts and varieties of extensively potential applications in medicine, agriculture, chemistry, materials, supramolecular sciences and so on.

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“…The synthesis of novel 1,2,4-triazole-5-thione derivatives and investigation of their biological activities have gained more importance in recent years. A survey of literature revealed their potential pharmacological activity profile as antibacterial (1-4), antifungal (5,6), antitubercular (7,8), antiviral (9,10), anticancer (11)(12)(13) and anticonvulsant (14,15). Besides the pharmacological significance of this heterocyclic ring system it is also an attractive scaffold to be constituted for chemical diversity.…”

Section: Introductionmentioning

confidence: 99%

Development of a New and Efficient Synthesis Method of 1,2,4-Triazole-5-Thione Derivatives

Abacı¹,

Rollas²,

Tatar³

2013

mpj

Self Cite

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3,4-Disubstituted-2,4-dihydro-5H-1,2,4-triazole-5-thiones were synthesized by a new one-pot, two-step synthesis method which was demonstrated to be superior than the current synthesis methods. The new method involves addition of alkyl/aryl isothiocyanates to substituted hydrazides in ethanol following the refluxing process of intermeadiate in 4N sodium hydroxide solution. According to our new synthesis procedure, reaction has gone to completion within 6 hours by higher product yields and reduced solvent usage.

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Synthesis of some novel thiourea derivatives obtained from 5-[(4-aminophenoxy)methyl]-4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones and evaluation as antiviral/anti-HIV and anti-tuberculosis agents

Cited by 193 publications

References 44 publications

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

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

Current Developments in the Syntheses of 1,2,4-Triazole Compounds

Development of a New and Efficient Synthesis Method of 1,2,4-Triazole-5-Thione Derivatives

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