scholarly journals Biological activity of the derivatives of 1,2,4-triazole

2018 ◽  
pp. 25-30
Author(s):  
T. V. Kravchenko ◽  
O. I. Panasenko ◽  
E. G. Knysh
Keyword(s):  
Biological Activity ◽  
Rapid Development ◽  
Heterocyclic Ring ◽  
Modern Medicine ◽  
Biologically Active ◽  
Literary Analysis ◽  
Professional Literature ◽  
Synthetic Drugs ◽  
Wide Range ◽  
Derivatives Of

The rapid development of modern medicine and pharmacy leads to an increase in synthetic drugs. Thus, in the professional literature says that one of the perspective directions are searching for new biologically active compounds including heterocyclic systems and the introduction of the latest in medical, pharmaceutical or veterinary practice. It is known that heterocyclic ring system 1,2,4-triazole moiety is promising for the synthesis of new active ingredients with various kinds of pharmacological actions. The aim of the study was the analysis of literature and patent sources over the past 10 years and the generalization of the results for certain types of biological activity of 1,2,4-triazole. Results of literary analysis show a wide range of biological activity of 1,2,4-triazole-3-tion. The data determine the relevance of further research of derivatives of 1,2,4-triazole in the actoprotective, antimicrobial, antifungal, antihypoxic, hypoglycemic, analgesic, antiinflammatory and others activity in order to find new highly effective in terms of biological substances that can form the basis of new medicines.

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.

Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Experimental Studies ◽  
New Drugs ◽  
Reduced Form ◽  
Free Form ◽  
Wide Range ◽  
On Line ◽  
Living Organisms ◽  
Derivatives Of

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.

Biological and medicinal application of Cucumis sativus Linn. – review of current status with future possibilities

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Anayatullah Khan ◽  
Anuradha Mishra ◽  
Syed Misbahul Hasan ◽  
Afreen Usmani ◽  
Mohd Ubaid ◽  
...  
Keyword(s):  
Cucumis Sativus ◽  
Cost Effective ◽  
Pharmacological Action ◽  
Modern Medicine ◽  
Current Status ◽  
Synthetic Drugs ◽  
Wide Range ◽  
Increasing Demand ◽  
Calcium Iron ◽  
Whole Plants

Abstract Objectives The increasing demand for herbal drugs for the human application is causing a growing demand for the cultivation of Medicinal Plants. This demand has developed because of cost-effective, plant-derived products rather than commercially available synthetic drugs. Cucumis sativus Linn. (Ver. Kheera) is a vegetable climber, species belongs to family Cucurbitaceae This species has a wide range of medicinal and biological applications thanks to its richness in carbohydrate, proteins, minerals (calcium, iron, magnesium, phosphorus, potassium, zinc) and secondary metabolites like alkaloids, tannins, flavonoids, saponins, and phenolic compounds These phytoconstituents may be responsible for allied therapeutic application. So, C. sativus possess wider applications for preventing certain ailments. Content The literature in various national and international journals and reports pertaining to the medicinal and nutritional uses were reviewed. The result revealed the current therapeutic applications of C. sativus whole plants other than the nutritional value. C. sativus pharmacological action includes antioxidant, anti-diabetic, UV protectant, hepatoprotective, gastroprotective, anti-helminthic, wound healing, antimicrobial, and anticancer. So, it could be useful for both preventive and additive therapy along with modern medicine for the better management of certain disorders. Summary and Outlook This review furnishes updated information about the phytoconstituents and their medicinal applications so that it can pose a path for the young researchers to do future findings.

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

2019 ◽  
pp. 28-44
Author(s):  
V. V. Parchenko
Keyword(s):  
Chemical Properties ◽  
Biological Properties ◽  
Modern Medicine ◽  
Toxic Substances ◽  
Triazole Derivatives ◽  
Synthetic Drugs ◽  
Physico Chemical ◽  
Methods Of Synthesis ◽  
Amino Derivatives ◽  
Derivatives Of

Modern medicine and pharmacy has at its disposal highly efficient synthetic drugs. Large extent of these drugs accounted for derivatives of 1,2,4-triazole. The purpose of the work was an attempt to summarize the literature in recent years related to the methods of synthesis and study of physico-chemical properties 3-thio- and 3-thio-4-amino derivatives of 1,2,4-triazole. Studies national scientists in recent years indicates prospects of the search in this direction, since this class of organic compounds is interest not only to scientists pharmaceutical, medical and veterinary field, but also among researchers of engineering, metallurgical and agricultural areas. 1,2,4-triazole derivatives are also widely used in practice for optical materials, photosensitizers are used as coloring agents, antioxidants, additives for fuels and oils, some of which are widely used as corrosion inhibitors for controlling various pests in agriculture. In addition, 1,2,4-triazole derivatives belong to the class low toxic or essentially non-toxic substances. The presence of a growing number of publications about methods of synthesis, reactions, physico-chemical and biological properties of 1,2,4-triazole, inspires scientists around the world search for perspective molecules of substituted 1,2,4-triazole. It should be noted that in spite of a sufficient amount of information about the derivatives of 1,2,4-triazole, some issues related to the generalization of data in the literature synthesis presented insufficient.

scholarly journals Synthesis of Optically Active Bicyclic Derivatives of Nitroimidazoles

Compounds ◽  
2021 ◽  
Vol 1 (3) ◽  
pp. 145-153
Author(s):  
Justyna Żwawiak ◽  
Lucjusz Zaprutko
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Biological Activity ◽  
Optically Active ◽  
Tuberculostatic Activity ◽  
Wide Range ◽  
Derivatives Of

Nitroimidazoles are characterized by a wide range of biological activity and many of them are used as therapeutics. Moreover, some bicyclic nitroimidazooxazoles show considerable potency against Mycobacterium tuberculosis. Some authors noticed that in the case of chiral derivatives of nitroimidazodihydrooxazoles, the (R) form shows a greater tuberculostatic activity than the (S) enantiomer. This work describes the procurement of new 12 enantiomeric bicyclic derivatives of nitroimidazole.

scholarly journals Structure and biological action of analogs and derivatives of biogenic polyamines

2021 ◽  
Vol 16 (4) ◽  
pp. 287-306
Author(s):  
O. S. Egorov ◽  
N. Yu. Borisova ◽  
E. Ya. Borisova ◽  
M. L. Rezhabbaev ◽  
E. Yu. Afanas’eva ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Action ◽  
Drug Formulation ◽  
Receptor Interaction ◽  
Cell Transport ◽  
Neuropsychiatric Diseases ◽  
Wide Range ◽  
Biogenic Polyamines ◽  
The Impact ◽  
Derivatives Of

Objectives. Biogenic polyamines are widely present in nature. They are characteristic of both protozoan cells and multicellular organisms. These compounds have a wide range of biological functions and are necessary for normal growth and development of cells. Violation of polyamine homeostasis can cause significant abnormalities in cell functioning, provoking various pathological processes, including oncological and neuropsychiatric diseases. The impact on the “polyamine pathway” is an attractive basis for the creation of many pharmacological agents with a diverse spectrum of action. The purpose of this review is to summarize the results of the studies devoted to understanding the biological activity of compounds of the polyamine series, comparing their biological action with action on certain molecular targets. Due to the structural diversity of this group of substances, it is impossible to fully reflect the currently available data in one review. Therefore, in this work, the main attention is paid to the derivatives, acyclic saturated polyamines.Results. The following aspects are considered: biological functionality, biosynthesis and catabolism, cell transport, and localization of biogenic polyamines in the living systems. Structural analogs and derivatives of biogenic polyamines with antitumor, neuroprotective, antiarrhythmic, antiparasitic, antibacterial, and other biological activities are represented; the relationship between biological activity and the target of exposure is reflected. It was found that the nature of the substituent, the number of cationic centers, and the length of the polyamine chain have a great influence on the nature of the effect.Conclusions. At present, the use of polyamine structures is restrained by cytotoxicity and nonspecific toxic effects on the central nervous system. Further research in the field of biochemistry, cell transport, and a deeper understanding of receptor interaction mechanisms will help making polyamines as the basis for potential drug formulation.

scholarly journals FLAVONOID COMPOUNDS FROM ARTEMISIA GLABELLA KAR. ET. KIR., SYNTHESIS ON THEIR BASIS AND BIOLOGICAL ACTIVITY

2018 ◽  
pp. 215-222
Author(s):  
Габиден (Gabiden) Маратович (Maratovich) Байсаров (Baysarov) ◽  
Айдана (Аjdana) Рахманиякызы (Rakhmaniyakyzy) Жуматаева (Zhumatayeva) ◽  
Гулим (Gulim) Кенесбековна (Kenesbekovna) Мукушева (Mukusheva) ◽  
Эльвира (El'vira) Эдуардовна (Eduardovna) Шульц (Shul'ts) ◽  
Роза (Roza) Батталовна (Battalovna) Сейдахметова (Seydakhmetova) ◽  
...  
Keyword(s):  
Biological Activity ◽  
Raw Materials ◽  
Hepatoprotective Activity ◽  
Biologically Active ◽  
Secondary Amines ◽  
Moderate Activity ◽  
Amino Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

As a result of complex chemical processing of medicinal raw materials of Artemisia glabella Kar. et Kir., including CO2 extraction and lactones isolation, we have investigated the chemical composition of flavonoids to select the biologically active ones and carry out modifications on their basis. Two flavonoids pectolinaringenin and cirsilineol have been isolated by partition chromatography from the secondary raw materials of Artemisia glabella Kar. et. Kir. and identified. To obtain new biologically active compounds, we have synthesized new amino derivatives of cirsilineol by the Mannich reaction with secondary amines (piperidine and N-methylpiperazine) in isopropanol with the presence of dimethylaminopyridine. In proton NMR spectrum of the synthesized compounds there are proton signals of the initial cirsilineol fragment; however, there is no N-8 proton signal, besides other signals typical for amines’ benzene ring have been observed at 1.53–3.90 ppm. It means that reaction occurred at the C-8 position of carbon in ring A. The synthesized compounds have been studied for various types of biological activity typical for this class, including hepatoprotective and anti-inflammatory activities. Amino derivatives of cirsilineol exhibit a moderate activity against HepG2 cell line, while cirsilineol at a dose of 5 mg/ml expresses a pronounced hepatoprotective activity. Moreover, all samples at a dose of 25 mg/kg show poor anti-inflammatory effects on the model of acute exudative reaction in vivo.

scholarly journals Algae Bioactive Constituents and Possible Role During COVID-19 Pandemic (A review)

2021 ◽  
Vol 30 (2) ◽  
pp. 16-22
Author(s):  
Sayed Rashad ◽  
Ghadir El-Chaghaby
Keyword(s):  
Bioactive Compounds ◽  
Biological Activities ◽  
Biologically Active ◽  
Bioactive Constituents ◽  
Algae Biomass ◽  
Synthetic Drugs ◽  
Pharmaceutical Applications ◽  
Active Chemical ◽  
Wide Range ◽  
Algal Products

Nowadays, the use of natural bio-products in pharmaceuticals is gaining popularity as safe alternatives to chemicals and synthetic drugs. Algal products are offering a pure, healthy and sustainable choice for pharmaceutical applications. Algae are photosynthetic microorganisms that can survive in different environmental conditions. Algae have many outstanding properties that make them excellent candidate for use in therapeutics. Algae grow in fresh and marine waters and produce in their cells a wide range of biologically active chemical compounds. These bioactive compounds are offering a great source of highly economic bio-products. The present review discusses the phytochemical and bioactive compounds present in algae biomass and their potent biological activities. The review focuses on the use of alga in therapy and their pharmaceutical applications with special reference to the possible preventive and therapeutic role of algae against COVID-19.

scholarly journals Synthesis of 5-hydroxy-10-R-benzo[a]phenazine-12-oxides by cyclization of 2-arylamino-1,4-naphthoquinone-1-oximes under the action of nitrating mixture

2020 ◽  
Vol 61 (2) ◽  
pp. 12-23
Author(s):  
Leonid M. Gornostaev ◽  
Keyword(s):  
Acetic Acid ◽  
Biological Activity ◽  
Nitrogen Oxide ◽  
Biologically Active ◽  
Alkyl Aryl ◽  
High Biological Activity ◽  
Fine Organic Synthesis ◽  
Wide Range ◽  
Fine Organic ◽  
Nitrosylsulfuric Acid

The synthesis of рolycyclic quinoid compounds, which exhibit a wide range of biological activity is one of the most promising and actively developing areas of the fine organic synthesis. Heterocyclic compounds including those that can be donors of nitrogen oxide NO occupy a special place among biologically active structures. These substances include a number of N-oxides, e.g., 1,2-diazet-1,2-dioxides, furoxanes and their benzo analogs, and N,N′-pyrazole dioxides. The reason for the high biological activity of N-oxides of nitrogenous heterocycles, which cannot easily generate nitrogen oxide NO may be their oxidative properties. Thus, N-oxides of nitrogenous heterocycles are of interest due to their high biological activity. We have developed an approach to the synthesis of 5-hydroxy-10-R-benzo[a]phenazine-12-oxides that contain the N-oxide fragment, which makes these compounds promising for studying their biological activity. We have demonstrated that the treatment of 2-arylamino-1,4-naphthoquinones with hydroxylamine in ethanol at 50-60 °С leads to selective oximation at position 1 and the formation of 2-arylamino-1,4-naphthoquinone-1-oximes. It has been shown that the interaction of 2-arylamino-1,4-naphthoquinone-1-oximes with the nitrating mixture in acetic acid results in the formation of 5-hydroxy-10-R-benzo[a]phenazine-12-oxides. Our work is a continuation of the study on the interactions of 2-arylamino-1,4-naphthoquinones and 4-arylamino-1,2-naphthoquinones with nitrosylsulfuric acid in acetic acid and the interaction of 2-alkyl(benzyl)amino-1,4-naphthoquinones with nitrosylsulfuric acid or nitrating mixture in acetic acid. The former reactions lead to the formation of 3-R-benzo[b]phenazine-6,11-dione-5-oxides and 9-R-benzo[a]phenazine-5,6-dion-7-oxides, respectively. The latter reaction leads to the formation of 2-alkyl(aryl)naphtho[2,1-d][1,3]oxazole-4,5-dione-4-oximes and 2-alkyl(aryl)-1-hydroxy-1H-naphtho[2,3-d]imidazole-4,9-dione as main products.

scholarly journals Synthesis and biological activity of Hepta-O-acetyl-1-O- (2-chloro-3-phenyl thio propyl)-β-D-maltose

2021 ◽  
Author(s):  
Lali Tabatadze ◽  
Neli Sidamonidze ◽  
Darejan Gulbani ◽  
Darejan Iremashvili
Keyword(s):  
Biological Activity ◽  
Biological Properties ◽  
Biologically Active ◽  
Pharmaceutical Chemistry ◽  
Chemical Research ◽  
Negative Effects ◽  
Physico Chemical ◽  
Bactericidal Properties ◽  
Wide Range ◽  
The Relationship

Carbohydrate derivatives are distinguished with wide range of biological activity which is proven by successful usage of preparations made of Carbohydrate based in different branches of pharmaceutical chemistry. As a result of research of Carbohydrate compounde, the relationship between unique structure and its chemical and biological properties has been studied. Input of bulk liphophilic adamantine moiety in the proved medications or biologically active molecule in most cases is improved molecule’s biological characteristic, drug’s lipopilycity and prolonged actin is enhanced, and at the same time toxicity and side negative effects is reduced.We studied the reactions of acetylaryl glycosides with phenylsulfonyl chloride in the presence of a benzoyl peroxide catalyst. A new sulfur-containing glucoside was synthesized: Hepta-O-acetyl-1-O-(2-chloro-3-phenyl thio propyl)-β-D-maltose. The bactericidal properties of β-O-(2-chloro-3-phenyl thio propyl)-D-maltose of the obtained product after deacetylation were studied. With the help of the com­­pu­ter program PASS (Prediction of Activity Spectra for Substance) onlaines were able to predict the range of activity of substances. The obtained result established correlations on bactericidal properties between biological activity and the intended biological activity. The structure of the synthesized compounds was determined by physico-chemical research methods.

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