Synthesis and Physicochemical Properties of Energetic 1,2,4,5‐Tetrazinyl Derivatives of 5‐Nitro‐2,4‐dihydro‐1,2,4‐triazol‐3‐one

2021 ◽  
Vol 6 (30) ◽  
pp. 7654-7662
Author(s):  
Gennady F. Rudakov ◽  
Ivan B. Kozlov ◽  
Nikolay V. Boev ◽  
Svetlana S. Zinchenko ◽  
Lyudmila Ya. Melnikova ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Derivatives Of

Chemical modification and Physicochemical properties of new derivatives 5-(thiophen-3-ilmethyl)-4-R1-1,2,4-triazole-3-thiol

2021 ◽  
pp. 4621-4629
Author(s):  
O.A. Bihdan ◽  
V.V. Parchenko
Keyword(s):  
Physicochemical Properties ◽  
High Reactivity ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Triazole Derivatives ◽  
Pharmaceutical Ingredients ◽  
Current Trends ◽  
Wide Range ◽  
Derivatives Of

Current trends in the search for new biologically active compounds among synthetic molecules have arguably proved a priority in studies of the heterocyclic 1,2,4-triazole system. For many years, 1,2,4-triazole derivatives remain the object of close attention of scientists of various scientific fields. The unique properties of 1,2,4-triazole derivatives include high reactivity, which allows different modification of this system, practical absence of toxicity of these derivatives and the presence of a wide range of biological, pharmacological properties, which in the complex provides the prerequisites for the creation of new biologically active compounds, and in the future, active pharmaceutical ingredients (AFI). The aim of our work is to investigate some transformations in a number of derivatives of 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiol, to study the physicochemical properties of the new synthesized compounds. A well-known fact remains the successful attempt of many scientists involved in the study of the heterocyclic 1,2,4-triazole system to synthesize potential biologically active compounds. The process of creating new molecules is very painstaking and requires considerable effort. The chemical approaches for the synthesis of the starting compounds required for further transformations are well known and described. Therefore, we used the corresponding N-R1-2 as intermediates for the synthesis of new 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiols appropriate ones were used N-R1-2-(2-(thiophen-3-yl) acetyl) hydrazinocarbothioamide.

scholarly journals The synthesis and physicochemical properties of new derivatives of 5-r-phenylamino-2-mercapto-1,3,4-thiadiazole

2016 ◽  
Vol 0 (1(85)) ◽  
pp. 24-28
Author(s):  
I. V. Sych ◽  
L. O. Perekhoda ◽  
Z. G. Ieromina ◽  
L. O. Grinevich ◽  
N. P. Kobzar ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Derivatives Of

Preparation and physicochemical properties of glycosylated derivatives of pea legumin

1990 ◽  
Vol 38 (8) ◽  
pp. 1700-1706 ◽  
Author(s):  
Daniele Caer ◽  
Alain Baniel ◽  
Muriel Subirade ◽  
Jacques Gueguen ◽  
Bernard Colas
Keyword(s):  
Physicochemical Properties ◽  
Derivatives Of

scholarly journals SYNTHESIS AND PHYSICOCHEMICAL PROPERTIES OF N-ACYL DERIVATIVES OF S-(2-METHYLQUINOLINE-4-YL)-L-CYSTEINE

2021 ◽  
Author(s):  
Luydmyla OMELYANCHIK ◽  
Oleksandr BRAZHKO ◽  
Viktoriia GENCHEVA ◽  
Iryna LABENSKA ◽  
Yuliіa PETRUSHA
Keyword(s):  
Physicochemical Properties ◽  
Derivatives Of ◽  
Acyl Derivatives

scholarly journals Synthesis, physicochemical properties and antigypoxic activity of some S-derivatives of 4-alkyl-5-(((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol

2020 ◽  
pp. 56-64
Author(s):  
E. O. Karpun ◽  
V. V. Parchenko
Keyword(s):  
Physicochemical Properties ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Acute Hypoxia ◽  
Spectral Parameters ◽  
Reference Drug ◽  
Mass Spectral ◽  
Biological Studies ◽  
Pharmacological Screening ◽  
Derivatives Of

Hypoxia is a discrepancy between the required energy of the cell in the mitochondrial oxidative phosphorylation system. The immediate cause of the deficiency is a decrease in the oxygen concentration in the mitochondria. Today there is a huge demand for the development of new anti-hypoxic drugs. t is known that 1,2,4-triazole compounds can have antimicrobial, anti-inflammatory, anti-hypoxic effects. Modification of the 1,2,4-triazole nucleus is a productive way to create original active molecules with a non-planar structure, for their binding to bio-target substrates. Derivatives of bis-1,2,4-triazoles may become potential compounds with anti-hypoxic action. The aim of our work was to synthesize new S-derivatives of 4-alkyl-5-(((3-(pyridine-4-yl)-1Н-1,2,4-triazole-5-yl)thio)methyl)-4Н-1,2,4-triazole-3-thiols, to investigate their physicochemical parameters using modern complex physicochemical research methods and to conduct primary pharmacological screening for anti-hypoxic activity in models of acute hypoxia with hypertension. The object of the study was the S-derivatives of 4-alkyl-5-(((3-(pyridine-4-yl)-1Н-1,2,4-triazole-5-yl)thio)methyl)-4Н-1,2,4-triazole-3-thiols. The structure of the synthesized compounds was confirmed by elemental analysis (CHNS), 1H NMR, the individuality of the molecules was proved by chromatographic mass spectral analysis. 1H NMR signals for substances are consistent with the proposed structure. The study of the anti-hypoxic activity of the got compounds of the series of S-substituted bis-1,2,4-triazoles was carried out on models of acute hypoxia with hypertension, where Mexidol (5%) 200 mg/kg as a reference drug. New S-derivatives of 4-methyl-5-(((3-(pyridine-4-yl)-1Н-1,2,4-triazole-5-yl)thio)methyl)-4Н-1,2,4-triazole-3-thiols (I a) and 4-ethyl-5-(((3-(pyridine-4-yl)-1Н-1,2,4-triazole-5-yl)thio)methyl)-4Н-1,2,4-triazole-3-thiols (I b) with acyl-aryl, acyl-alkyl and alkyl substituents. We studied their spectral parameters, physicochemical properties in the conditions of GC/MS, elemental analysis, 1H NMR spectroscopy. According to the results of biological studies on the anti-hypoxic effect, it was found that 1-((4-ethyl-5-(((3-(pyridine-4-yl)-1H-1,2,4-triazole-5-yl)thio)methyl)-4H-1,2,4-triazole-3-yl)thio)propane-2-one is a compound that exceeds the anti-hypoxic activity of Mexidol and increases the lifespan of rats by 1.0% relative to the reference drug.

scholarly journals Synthetic derivatives of genistein, their properties and possible applications.

2010 ◽  
Vol 57 (1) ◽  
Author(s):  
Aleksandra Rusin ◽  
Zdzisław Krawczyk ◽  
Grzegorz Grynkiewicz ◽  
Agnieszka Gogler ◽  
Jadwiga Zawisza-Puchałka ◽  
...  
Keyword(s):  
Drug Development ◽  
Physicochemical Properties ◽  
Clinical Application ◽  
Current Knowledge ◽  
Chemical Reactivity ◽  
Food Supplement ◽  
Basic Information ◽  
Chemopreventive Agent ◽  
Synthetic Derivatives ◽  
Derivatives Of

Genistein, the principal isoflavone constituent of soybean, attracts much attention as a natural molecule with significant affinity towards targets of potential medicinal interest, but also as a food supplement or prospective chemopreventive agent. Since its physicochemical properties are considered suboptimal for drug development, much effort has been invested in designing its analogs and conjugates in hope to obtain compounds with improved efficacy and selectivity. The aim of this article is to summarize current knowledge about the properties of synthetic genistein derivatives and to discuss possible clinical application of selected novel compounds. Some basic information concerning chemical reactivity of genistein, relevant to the synthesis of its derivatives, is also presented.

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