scholarly journals Synthesis and structural features of 5-(4-(tert-butyl) phenyl)-4-((R)amino)-4H-1,2,4-triazole-3-thiols

2018 ◽  
pp. 60-65
Author(s):  
I. I. Aksyonova-Seliuk ◽  
O. I. Panasenko ◽  
E. G. Knysh
Keyword(s):  
Chemical Structure ◽  
Chemical Properties ◽  
Biologically Active ◽  
Physical And Chemical Properties ◽  
Tert Butyl ◽  
New Compounds ◽  
Physical And Chemical ◽  
Derivatives Of ◽  
Active Substances ◽  
And Chemical Properties

Chemistry of heterocyclic compounds is one of the most popular sector in organic chemistry. Scientists allocate among them a class of derivatives of 1,2,4-triazole. This class of compounds attracts attention his broad spectrum of biological activity. There are antiviral, anti-inflammatory, anti-tubercular, antimicrobial, antioxidant, actoprotective, anti-cancer and other activities. The derivatives of 1,2,4-triazole have one more important advantage. It is low toxicity. This properties do this class of derivatives promising for researches their chemical structure and biological activity and purposeful search of biologically active substances. The purpose of the work is synthesis of 5-(4-(tert-butyl)phenyl)-4-((R)amino)-4H-1,2,4-triazoles-3-thiols from appropriate ylidene derivatives of 4-amino-5-(4 (tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol and research of their physical and chemical properties. The objects of research were 10 new compounds, derivatives of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol. These compounds are the crystal substances which are odorless, insoluble in water and soluble in organic solvents. Investigation of the physical and chemical properties of this compounds was carried out according to the methods listed in the State Pharmacopoeia of Ukraine. The melting temperature of synthesized compounds was determined by device OptiMelt Stanford Research Systems MPA100. The structure of the compound was confirmed by 1H-NMR spectroscopy (Mercury 400) and gas chromatography-mass spectrometry (Agilent 1260 Infinity HPLC). 10 new compounds, derivatives of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol, were synthesized in a study. The chemical structure of the new compounds was confirmed by modern instrumental methods of analysis. Results of the done work can be use in the future search of biologically active substances.

scholarly journals Synthesis, physical and chemical properties of 5-(phenoxymethylene)-4-R-1,2,4-triazol-3-thiones derivatives, which contain alkyl- and arylnitrile fragments

2018 ◽  
pp. 52-58
Author(s):  
Yu. M. Kucheryavyi ◽  
A. G. Kaplaushenko
Keyword(s):  
Chemical Properties ◽  
Biologically Active ◽  
Physical And Chemical Properties ◽  
Chemical Methods ◽  
The Core ◽  
Physical And Chemical ◽  
Tumor Drugs ◽  
Derivatives Of ◽  
Active Substances ◽  
And Chemical Properties

Ukraine takes the second place in Europe for the dissemination of cancer. Ukrainian pharmaceutical market practically doesn’t have domestic anti-tumor drugs. That’s why, many scientists of pharmaceutical industry work in this direction.  The searching of biologically active substances among derivatives of 1,2,4-triazole is actually for today. Anastrozole and Letrozole are enough known like anti-tumor drugs which contain in their structures the core of 1,2,4-triazole and nitrile groups. The aim of our work is purposeful synthesis a number of new highly effective compounds 2-((5-(phenoxymethylene)-4-R-4H-1,2,4-triazole-3-yl)thio)acetonitriles and 2-, 3-, 4-(((5-(phenoxymethylene)-4-R-4H-1,2,4-triazole-3-yl)thio)methyl)benzo-nitriles, research of its physical and chemical properties. The 5-(phenoxymethylene)-4-R-1,2,4-triazole-3-thiones, which contain alkyl- and arylnitrile groups has been synthesized and its effective methods obtaining have been set. The structure of synthesized compounds has been confirmed by modern complex of physical and chemical methods of analysis. The synthesized compounds with alkyl- and arylnitrile functional groups will become the basis for further modification of the structure to increase results or expand the range of the biological activity.

scholarly journals Some transformations and physicochemical properties of new S-substituted 5-thiophene-(3-ylmethyl)-4R-1,2,4-triazole-3-thiols

2021 ◽  
pp. 50-56
Author(s):  
А. В. Хільковець
Keyword(s):  
Alkaline Medium ◽  
Chemical Properties ◽  
Monochloroacetic Acid ◽  
Esterification Reaction ◽  
Physical And Chemical Properties ◽  
Analysis Methods ◽  
New Compounds ◽  
Physical And Chemical ◽  
Derivatives Of ◽  
And Chemical Properties

Nitrogen-containing heterocyclic compounds are widely represented in modern organic chemistry. A special place among the huge number of substances presented is occupied by derivatives of 1,2,4-triazole due to their uniqueness and prospects. In recent years, these derivatives have remained the object of close attention of both synthetic chemists and researchers engaged in the search for new biologically active substances of a wide spectrum of action, the synthesis of optical materials, dyes, corrosion inhibitors, veterinary drugs, etc. It is known from the literature that the combination of the aromatic heterocycle of thiophene and 1,2,4-triazole is a promising area for research. The result of such combinations is a number of compounds obtained with fairly high yields and a wide range of activities. Thus, further chemical modification of 1,2,4-triazole derivatives by additional administration of a typical thiophene pharmacophore is an urgent task. The aim of the study is to obtain new compounds in a number of S-substituted 5-thiophene-(3-ylmethyl)-4R-1,2,4-triazole-3-thiols and study their physico-chemical properties using complex analysis methods. The study of the physical and chemical properties of the compounds obtained was carried out according to methods that meet the standards of the state pharmacopoeia of Ukraine. The synthesis of new compounds was carried out according to generally accepted methods. The previously obtained 5-thiophene-(3-ylmethyl)-4h-1,2,4-triazole-3-thiol and 5-thiophene-(3-ylmethyl)-4-phenyl-1,2,4-triazole-3-thiol were used as starting compounds. Preparation of thioethanones was performed in an alkaline medium in the presence of methanol. The acids were obtained in an alcohol-alkaline medium with the addition of monochloroacetic acid. To obtain esters, two conventional methods were used. The first method is based on the alkylation in an alkaline-alcohol medium of the starting thiols with isopropyl ester of monochloroacetic acid. The second method is the classical esterification reaction. To confirm the structure and study of the physical and chemical properties, all the resulting compounds were crystallized. As a result, some new compounds that were not previously described were obtained, namely: thioethanones, thioacetamides, thioacetic acids, thioacetates, and a number of other thiopo-derivatives of these initial compounds. The structure and individuality of the obtained molecules were confirmed by elemental analysis (CHNS), IR and 1H NMR spectra. A number of new S-derivatives of 5-thiophene-(3-ylmethyl)-4R-1,2,4-triazole-3-thiols have been obtained. The physical and chemical properties of the obtained compounds are determined and their structure is confirmed using modern analysis methods. Some compounds will be transferred for further research.

A Facile Synthesis of substituted Trifluoromethyl piperidines with diversify functionalization

2021 ◽  
Vol 18 ◽  
Author(s):  
Wahid Bux Jatoi ◽  
Ashique Hussain Balouch ◽  
Mazhar Iqbal Khaskheli ◽  
Nafeesa Khatoon Shahani ◽  
Qurat-Ul-Ain Shaikh ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Biologically Active ◽  
Physical And Chemical Properties ◽  
Great Tendency ◽  
Facile Synthesis ◽  
Physical And Chemical ◽  
Derivatives Of ◽  
Aromatic Heterocyclic ◽  
Active Natural ◽  
And Chemical Properties

: Piperidine-based alkaloids are undoubtedly an important class of biologically active natural products. When a unique group like trifluoromethyl (Tfm) is added to an active compound, it significantly ameliorates its bioactivity, bioavailability, physical and chemical properties. Many fluorination and trifluoromethylation methods have been reported. In the present paper, we have shown that among all other trifluoromethylation pathways, Mannich reaction also has the great tendency to introduce a Tfm group in a saturated or aromatic heterocyclic compound. Applications of this reaction are elaborated in preparing several derivatives of piperidine base alkaloids with trifluoromethyl at α-position. Furthermore, the substitution at C-4 and C-6 was successfully achieved with variety of saturated and aromatic groups.

scholarly journals Two (Sulfone-Amidosulphonyl)-Amides Derived from N-(P-Amidobenzoyl)-L-Glutamine; Optimized Synthesis and Toxicity Study

2016 ◽  
Vol 22 (3) ◽  
pp. 609-615
Author(s):  
Corina Cheptea ◽  
Andreea Celia Benchea ◽  
Marius Gaina ◽  
Dana Ortansa Dorohoi ◽  
Valeriu Sunel
Keyword(s):  
Mechanical Characterization ◽  
Chemical Properties ◽  
Quantum Mechanical ◽  
Physical And Chemical Properties ◽  
Physical Conditions ◽  
Relevant Variables ◽  
New Compounds ◽  
Physical And Chemical ◽  
Derivatives Of ◽  
And Chemical Properties

Abstract Two derivatives of glutamine were synthesized and the most convenient physical conditions for obtaining reactions were established in factorial experiments with temperature and time of reactions considered as relevant variables. A quantum-mechanical characterization for the new compounds was performed by using HyperChem 8.0.6 Programs and their physical and chemical properties were theoretically estimated. The toxicity of two new compounds was experimentally determined.

scholarly journals Synthesis of monoketo and monohydroxy eicosanoic acids and esters with substituents at odd-numbered (3-13) carbons

2002 ◽  
Vol 67 (7) ◽  
pp. 473-480 ◽  
Author(s):  
Hulya Çelik
Keyword(s):  
Nmr Spectroscopy ◽  
High Purity ◽  
1H Nmr Spectroscopy ◽  
Methyl Esters ◽  
Chemical Properties ◽  
Physical And Chemical Properties ◽  
Keto Acids ◽  
Physical And Chemical ◽  
Derivatives Of ◽  
And Chemical Properties

In this study, monoketo and monohydroxy eicosanoic acids and their methyl esters with the position of the substituent on odd numbered carbon atoms from 3 to 13 were synthesized with high purity. Furthermore, the semicarbazone and anilide derivatives of the obtained keto acids were prepared. They were characterized by TLC, IR and 1H-NMR spectroscopy and their physical and chemical properties were established.

scholarly journals Analysis of oxidation degree of graphite oxide and chemical structure of corresponding reduced graphite oxide by selecting different-sized original graphite

RSC Advances ◽  
2018 ◽  
Vol 8 (31) ◽  
pp. 17209-17217 ◽  
Author(s):  
Lu Shen ◽  
Lihua Zhang ◽  
Kui Wang ◽  
Lijing Miao ◽  
Qiaofeng Lan ◽  
...  
Keyword(s):  
Graphite Oxide ◽  
Chemical Structure ◽  
Chemical Properties ◽  
Thermal Reduction ◽  
Physical And Chemical Properties ◽  
Oxidation Degree ◽  
Reduced Graphite Oxide ◽  
Physical And Chemical ◽  
And Chemical Properties

The thermal reduction of GO is the most commonly used strategy for preparation of rGO, and the oxidation degree of GO would influence the chemical structure of prepared rGO, thereby affecting its physical and chemical properties.

PERBANDINGAN PELARUT ETANOL DAN AIR PADA PEMBUATAN EKSTRAK UMBI BAWANG TIWAI (Eleutherine americana Merr) MENGGUNAKAN METODE MASERASI

2017 ◽  
Vol 1 (2) ◽  
pp. 149
Author(s):  
Hayatus Sa'adah ◽  
Henny Nurhasnawati
Keyword(s):  
Medicinal Plant ◽  
Chemical Properties ◽  
Physical And Chemical Properties ◽  
Phytochemical Screening ◽  
Water As Solvent ◽  
Physical And Chemical ◽  
Eleutherine Americana ◽  
Solvent Optimization ◽  
Active Substances ◽  
And Chemical Properties

Bawang tiwai (Eleutherine americana Merr) is one kind of medicinal plant. To obtain an active substances with good physical and chemical properties, it is needs to do optimization of making extracts, one with solvent optimization. Type of solvent will determine the types of extracted substances in accordance with the polarity. On this research, extraction of bawang tiwai bulbs simplicia by maceration method using ethanol and water as solvent. This research is an experimental research with varying ethanol and water in a three comparison solvent that is water, ethanol, and mixture of water-etanol, then the yields is calculated. Furthermore, the data were analyzed statistically using ANOVA program to determine significant differences in the three yields. In each extract was conducted phytochemical screening to determine the content of secondary metabolites. The results showed significant differences in the yield of bawang tiwai extract with three treatments and two repetitions. The results of average yields using water as solvent is 8.75%, ethanol 5.3%; and water-etanol 8.31%

scholarly journals FORMULASI DAN UJI PELEPASAN KRIM EKSTRAK ETANOL DAUN JAMBU BIJI DENGAN POTENSI ANTIJERAWAT

Jurnal Kimia ◽  
2020 ◽  
pp. 119
Author(s):  
N. P. Y. A. Dewi ◽  
N. L. G. W. Pebriani ◽  
P. A. Duarsa ◽  
P. C. I. Warnaya ◽  
I. D. A. A. D. Candraningrat ◽  
...  
Keyword(s):  
Stearic Acid ◽  
Chemical Properties ◽  
Ethanol Extract ◽  
Physical And Chemical Properties ◽  
Guava Leaves ◽  
Guava Leaf ◽  
Optimum Formula ◽  
Physical And Chemical ◽  
Active Substances ◽  
And Chemical Properties

Guava leaves contain quercetin which can inhibit the growth of Propionibacterium acne. Thus, guava leaves have the potential to be anti-acne. Based on the benefits of guava leaves, it is necessary to formulate the ethanol extract of guava leaves in cream preparation and its characterization as well as to know the rate of releasing active substances. Preparation and standardization of guava leaf simplicia was carried out. After that, maceration, standardization and phytochemical screening of guava leaf ethanol extract were done. Positive extracts containing flavonoids were formulated into cream preparation. The concentration of stearic acid as emulgator of 14% and 18% was optimized. The formula was tested for physical and chemical properties such as organoleptic, spreadability, adhesion, viscosity and pH. The optimum formula was characterized using Franz diffusion test to determine the release of the active substance. The results showed that concentration of stearic acid as emulgator influenced the physical and chemical properties of the cream. Based on the results of this study it could be concluded that the optimum formula was stearic acid concentration of 14% with the release active substances for 3 hours of 2,5882 mg. Keywords: Guava leaves, acne, cream, stearic acid, diffusion

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