Synthesis methods of 1,2,4-triazole-3-thiones: review DOI Creative Commons
Yuliia Frolova, А. Г. Каплаушенко,

T. V. Ihnatova

et al.

Current issues in pharmacy and medicine science and practice, Journal Year: 2024, Volume and Issue: 17(2), P. 187 - 196

Published: June 14, 2024

1,2,4-Triazole-containing compounds are unique heterocyclic present in an array of pharmaceuticals and biologically important used drug-discovery studies against cancer cells, microbes, various types diseases the human body. The aim study was to analyze detail combine available literature materials reactions associated with formation different classes derivatives 1,2,4-triazole-3-thione their physical-chemical properties. Various innovative methods have been proposed explored for synthesizing 1,2,4-triazole compounds, each distinct applications potential medicinal benefits. When analyzing outcomes aimed at obtaining new 1,2,4-triazole-3-thiones, it’s crucial recognize multiple stages involved synthesis. These typically include esterification carboxylic acids, hydrazinolysis, carbothioamides, thiones through alkaline cyclization. Subsequently, involving S-function conducted, leading 1,2,4-triazole. by a team scientists introduced novel method imidazolyl- imidazole-1,2,4-triazoles, targeting design safer analgesic anti-inflammatory agents. Moreover, researchers successfully synthesized 3-[2-(5-thio-4-aryl-4H-1,2,4-triazole-3-yl)ethyl]quinoxalin-2(1H)-one, N-(3-thio-5-aryl-[1,2,4]triazole-4-yl)acylamides, 5-alkylthio-4-amino-3-(5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine-2-thiomethyl)-1,2,4-triazole 3-(5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine-2-thiomethyl)-6-aryl-5,6-dihydrogen-1,2,4-triazole-[3,4-b]-1,3,4-thiadiazole, 5,5’-(alkyldiyl-bis(sulfandiyl))bis(N-(arylidene)-3-thiophen-2-ylmethyl)-4H-1,2,4-triazole-4-amines, 3-(arylsulfonyl)-4-phenyl-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazole, expanding scope 1,2,4-triazole-based, pharmacological activities. Furthermore, synthesis molecules containing two benzole rings has gained traction, offering avenues drug development. Mannich bases were from corresponding reaction N-methylpiperazine or N-phenylpiperazine dimethylformamide presence formaldehyde. Additionally, salts derived highlights its importance pharmaceutical formulations, focusing on both organic inorganic therapeutic applications. Conclusions. analysis above-mentioned publications indicates that search active among 1,2,4-triazole-3-thiones is promising. Many exhibit wide spectrum biological activity little toxicity.

Language: Английский

Synthesis and In Vitro Evaluation of Triazole‐Based N‐(Substituted phenyl)‐5‐[(benzyl)‐4‐(phenyl)‐4H‐1,2,4‐triazol‐3‐ylthio]acetamides as Potent Acetylcholinesterase Inhibitors DOI
Faisal Shahzad, Sabahat Zahra Siddiqui, Azizur Rehman

et al.

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(16)

Published: April 1, 2025

Abstract The aim of this study was to design and evaluate the potential some new acetylcholinesterase (AChE) inhibitors, encompassing biologically important acetamides, 1,2,4‐triazole moieties structural amalgamation. A series N ‐(substitutedphenyl)‐[5‐(benzyl‐4‐(phenyl‐4 H ‐1,2,4‐triazol‐3‐ylthio)]acetamides ( 8a‐l ) synthesized through multistep synthetic protocol their structures were elucidated by modern contemporary spectral techniques, that is, IR, EI‐MS, 1 H‐NMR, 13 C‐NMR. in vitro AChE inhibitory activity compounds showed promising results ranged from IC 50 = 0.017 ± 0.008 7.518 0.241 µM as compared standard neostigmine methyl sulfate (IC 2.039 0.051 µM). Among novel molecules, compound 8j displayed most potent kinetics mechanism analyzed Lineweaver‐Burk Plots revealed inhibited enzyme competitively K i Furthermore, computational analysis also performed provide insights into binding interactions between enzymes' active sites, revealing key features responsible for high affinity. These findings suggest acetamide‐triazole derivatives are interesting candidates inhibition, providing possible avenues therapeutic interventions neurodegenerative diseases like alzheimer's disease.

Language: Английский

Citations

0
Synthesis of Novel 1,2,4-Triazole Derivatives of N-Benzyl-5-nitroisatin: Anticancer Activity, Anti-oxidant Activity, and Molecular Design DOI
Hala Ayad Mohamed Rasheed, Suaad M. H. Al-Majidi

Organic Preparations and Procedures International, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 13

Published: June 21, 2024

Language: Английский

Citations

1
Synthesis methods of 1,2,4-triazole-3-thiones: review DOI Creative Commons
Yuliia Frolova, А. Г. Каплаушенко,

T. V. Ihnatova

et al.

Current issues in pharmacy and medicine science and practice, Journal Year: 2024, Volume and Issue: 17(2), P. 187 - 196

Published: June 14, 2024

1,2,4-Triazole-containing compounds are unique heterocyclic present in an array of pharmaceuticals and biologically important used drug-discovery studies against cancer cells, microbes, various types diseases the human body. The aim study was to analyze detail combine available literature materials reactions associated with formation different classes derivatives 1,2,4-triazole-3-thione their physical-chemical properties. Various innovative methods have been proposed explored for synthesizing 1,2,4-triazole compounds, each distinct applications potential medicinal benefits. When analyzing outcomes aimed at obtaining new 1,2,4-triazole-3-thiones, it’s crucial recognize multiple stages involved synthesis. These typically include esterification carboxylic acids, hydrazinolysis, carbothioamides, thiones through alkaline cyclization. Subsequently, involving S-function conducted, leading 1,2,4-triazole. by a team scientists introduced novel method imidazolyl- imidazole-1,2,4-triazoles, targeting design safer analgesic anti-inflammatory agents. Moreover, researchers successfully synthesized 3-[2-(5-thio-4-aryl-4H-1,2,4-triazole-3-yl)ethyl]quinoxalin-2(1H)-one, N-(3-thio-5-aryl-[1,2,4]triazole-4-yl)acylamides, 5-alkylthio-4-amino-3-(5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine-2-thiomethyl)-1,2,4-triazole 3-(5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine-2-thiomethyl)-6-aryl-5,6-dihydrogen-1,2,4-triazole-[3,4-b]-1,3,4-thiadiazole, 5,5’-(alkyldiyl-bis(sulfandiyl))bis(N-(arylidene)-3-thiophen-2-ylmethyl)-4H-1,2,4-triazole-4-amines, 3-(arylsulfonyl)-4-phenyl-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazole, expanding scope 1,2,4-triazole-based, pharmacological activities. Furthermore, synthesis molecules containing two benzole rings has gained traction, offering avenues drug development. Mannich bases were from corresponding reaction N-methylpiperazine or N-phenylpiperazine dimethylformamide presence formaldehyde. Additionally, salts derived highlights its importance pharmaceutical formulations, focusing on both organic inorganic therapeutic applications. Conclusions. analysis above-mentioned publications indicates that search active among 1,2,4-triazole-3-thiones is promising. Many exhibit wide spectrum biological activity little toxicity.

Language: Английский

Citations

0