Synthesis, physico-chemical properties of 3-thio and 3-thio -4-amino derivatives of 1,2,4-triazole

Парченко, В. В.

doi:10.32352/0367-3057.2.15.01

Cited by 6 publications

(13 citation statements)

References 12 publications

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“…Добре вiдомо, що похiднi 1,2,4-триазолу мають широкий спектр бiологiчних властивостей, виявляючи водночас незначну токсичнiсть [1,2]. Оригінальне моделювання похідних 1,2,4-триазолу дає змогу одержувати нові молекули з унікальними властивостями [3,4].…”

Section: в с т у пunclassified

Development of industrial production technology with determination of the quality of a soft medicine «Vetmikoderm» for veterinary

Оглоблiна,

Бушуєва,

Мартинишин

et al. 2023

Farm Zh

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It is well known, that 1,2,4–triazole derivatives have a wide range of biological properties, showing little toxicity. Original modeling of 1,2,4-triazole derivatives allows obtaining new molecules with unique properties. Such purposeful changes in molecules are popular among many scientists because they make it possible to obtain compounds with «improved» properties. Such a compound was the substance (4-((5-(decylthio)-4-methyl-4H-1,2,4-triazol-3-yl)-methyl)morpholine with the prospect of creating a mild medicinal product – liniment «Vetmikoderm». The main advantage of these medicinal forms is a low traumatic effect on damaged tissue, creating maximum contact with the wound surface, etc. It has been proven, that the antimicrobial agents available on the veterinary drugs’ market, including those ones in the form of ointments, gels and liniments, are characterized by the fact that they do not always stimulate tissue regeneration processes. Medicines with the ability to improve wound healing, as a rule, have minor antiseptic properties. Under these circumstances, the search, development and introduction of the medicines that have antimicrobial and antifungal action is an extremely urgent issue of modern veterinary medicine. The aim of our research was to study the technological aspects and manufacturing features, the substantiation of the composition, the analysis of the soft medicinal form of the drug «Vetmikoderm». During the research, the appearance, transparency, and thickness of the drug were determined. APHI identification was carried out with the determination of its content by the gas chromatography’s method. The external standard method was used. Microbiological purity (bacteria, yeast and mold fungi (in total), the presence of bacteria of the Enterobacteriaceae family, Staphylococcus aureus and Pseudomonas aeruginosa) was determined in accordance with the requirements of the SPHU by the membrane filtration method. Sterile soy–casein agar was used to determine the total number of aerobic bacteria. Determination of harmlessness was carried out according to the «abnormal toxicity» indicator. On the basis of the conducted research, the technological aspects and manufacturing features, substantiation of the composition, quantitative and qualitative analysis of the «Vetmikoderm» liniment were determined, which ensures the possibility of the medicinal form’s obtaining in industrial conditions. The proposed methods of the medicinal form’s analysis are characterized by sensitivity and reproducibility.

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Section: в с т у пunclassified

Development of industrial production technology with determination of the quality of a soft medicine «Vetmikoderm» for veterinary

Оглоблiна,

Бушуєва,

Мартинишин

et al. 2023

Farm Zh

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“…Among the variety of known organic compounds, the heterocyclic system of 1,2,4-triazole deserves special attention, as it has been at the center of research for decades [1,2,5]. The 1,2,4-triazole cycle has unique properties, which make it a very attractive target for research [3,4].…”

Section: Original Researchmentioning

confidence: 99%

Diuretic activity of some 4- and 3-thio-substituted 1,2,4-triazoles with fluorophenyl fragments

et al. 2023

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Diuretics increase the volume of urine and sodium excretion, and therefore are often used to remove excess fluid from the body during various diseases, including hypertension, heart and kidney failure, nephrotic syndrome, cirrhosis, etc. Until now, a wide range of diuretics is known, but none of them is completely safe and has a number of side effects. The aim of the work is to investigate the diuretic activity of 1,2,4-triazole derivatives containing fluorophenyl substituents at the fifth position of the 1,2,4-triazole fragment, as well as to establish the relationship between “chemical structure and diuretic action” among derivatives 1,2,4-triazole. Materials and methods. To study the effect on kidney function, six groups of animals with seven rats each were used. When studying water diuresis, rats were kept on a constant diet with free access to water. Before water loading (5 % of body weight), rats were fasted for 2 hours without food and water. Since all tested compounds were insoluble in water, they were administered orally as an aqueous suspension stabilized with Tween-80. The compounds were administered at a dose of 1/10 LD50. Results. The diuretic activity of 28 new compounds of a number of substituted 1,2,4-triazole-3-thiols, which according to their chemical structure belong to different classes of compounds, was investigated. Conclusions. Analysis of the results of diuretic activity indicates that there are a number of compounds whose activity is higher than hypothiazide, as well as a compound that exceeds the activity of furosemide.

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“…Derivatives of 1,2,4-triazole have a wide range of effects and can exhibit diverse activity. (Danilchenko et al, 2015, Kumar et al, 2013, Parchenko, 2012, Patel et al, 2013, Pattan et al, 2012. The actoprotective activity of some derivatives of 1,2,4-triazole has already been investigated (Salionov et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

Derivatives of 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-4-amines as increasing efficiency substances

Сафонов

2018

Indonesian J. Pharm.

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In today's society, especially in eastern countries such as China, Japan etc., the problem of fatigue and even death at work is acute. One of the solution to this problem is complex therapy with increasing efficiency drugs. Derivatives of 1,2,4-triazole have already proven themselves as potential compounds for pharmacological correction of fatigue. Compounds were synthesized at the Department of toxicological and inorganic chemistry ZSMU. Using method of forced swimming on a group of white nonlinear rats activity of anti-fatigue of the compounds were analyzed. Having analyzed the data of pharmacological correction of fatigue for 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4triazol-4-amines, it should be noted that this series of compound do not show anti-fatigue effect. Introduction in molecule 3-(nonylthio)-5-(thiophen-2-ylmethyl)-4H-1, 2, 4-triazol-4-amine 4-fluorbenzylidene, 4-(dimethylamino) benzylidene, 4methoxybenzylidene, 2-chloro-6-fluorobenzylidene radicals lead to increase actoprotective effect. The most active compound is N-(2-chloro-6-fluorobenzylidene)-3-(nonylthio)-5-(thiophen-2ylmethyl)-4H-1, 2, 4-triazol-4-amine which exceeds the standard (riboxin).

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Synthesis, physico-chemical properties of 3-thio and 3-thio -4-amino derivatives of 1,2,4-triazole

Cited by 6 publications

References 12 publications

Development of industrial production technology with determination of the quality of a soft medicine «Vetmikoderm» for veterinary

Development of industrial production technology with determination of the quality of a soft medicine «Vetmikoderm» for veterinary

Diuretic activity of some 4- and 3-thio-substituted 1,2,4-triazoles with fluorophenyl fragments

Derivatives of 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-4-amines as increasing efficiency substances

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