SYNTHESIS OF 3- (1,1-DIOXIDOTHIETAN-3-YL) -6-METHYLURACIL AND HYDRAZONE DERIVATIVES

2021 ◽  
pp. 181-189
Author(s):  
Melnikov A.S. ◽  
Meshcheryakova S.A.
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Statistical Processing ◽  
Biologically Active ◽  
High Biological Activity ◽  
Treatment And Prevention ◽  
Methods Of Synthesis ◽  
New Compounds ◽  
Derivatives Of

Uracil derivatives containing various N1, N3 substituents are characterized by various pharmacological and biological activities. Since the beginning of the XXI century, among them, new biologically active substances have been discovered that have pronounced antiparasitic, antibacterial, antioxidant properties. Known that modern methods of treatment and prevention of many diseases involve the inclusion of substances that have the ability to stimulate immune processes. Such compounds, in particular, include derivatives of nucleoside bases with high biological activity. Derivatives of 6-methyluracil containing a hydrazone system are widely studied in the treatment of Alzheimer's disease, antifungal, antiviral, antianginal, anti-eczema and other types of activity. The study of the alkylation of 6-methyluracil, which contains hydrazone systems in the role of pharmacophore fragments, is one of the topical trends in the synthesis of new chains of biologically active compounds. Purpose: For this purpose, we studied the alkylation of 6-methyl-3- (1,1-dioxidothietan-3-yl) pyrimidin-2,4 (1H, 3H)-dione with 1-chloropropan-2-one and the interaction of the resulting N1- 2-oxopropyl derivative with various hydrazines. Materials and Methods: The individuality of the new compounds was confirmed by the method of thin layer chromatography and determination of the melting point. The structure of the synthesized substances was confirmed by elemental analysis and NMR spectroscopy. Statistical data processing was carried out using variational analysis using the STATISTICA 8.0 software package. Student's test was chosen as a criterion for the representativeness of statistical processing. A preliminary analysis of toxicity and types of potential biological activity was carried out in silico using the resources of the Internet platform Way2Drag. Conclusions: Methods of synthesis have been developed and the most probable types of biological and pharmacological influence have been statistically processed, proceeding from the value of the probability of being active and the probability of inertness. Based on the analysis of data, modeled types of biological activity, some patterns of "structure-activity" are determined. In the conclusion, further directions of research are identified.

scholarly journals Synthesis and Characterization of New Compounds Derived from Pyrrolidine-2-One and Evaluation of their Biological Activities

2020 ◽  
Vol 23 (4) ◽  
pp. 5-12
Author(s):  
Nadia A. Betti ◽  
◽  
Redha Ib. Hussain ◽  
Sahar Ab. Kadhem ◽  
Abdul Jabar Kh. Atia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Mass Spectrum ◽  
Biological Activities ◽  
The Other ◽  
Synthesis And Characterization ◽  
E Coli ◽  
Ft Ir ◽  
New Compounds ◽  
Derivatives Of

New derivatives of pyrrolidine-2-one have been prepared by lactamization of -butyrolactone GBL with hydrazine hydrate (NH2NH2(80%)) to afford (1-aminopyrrolidin-2-one) which undergo many reactions to prepare the other derivatives. The prepared derivatives were determined by utilizing their FT-IR,1H-NMR and some by Mass spectrum. These derivatives were evaluated biologically against (Staphylococcus aureusand E. coli).Some of these derivatives exhibited good biological activity against one or both kind of bacteria while some exhibited no biological activity at all.

scholarly journals NEW APPROACHES TO SYNTHESIS OF HETEROCYCLIC DERIVATIVES OF PYRIDINE CARBOXYLIC ACIDS, ACRIDINE AND PYRAZOLONE

2021 ◽  
Vol 91 (1) ◽  
pp. 65-85
Author(s):  
D. V. Kazak ◽  
E. A. Dikusar ◽  
S. G. Stepin
Keyword(s):  
Biological Activity ◽  
Chemical Properties ◽  
Biologically Active ◽  
Pharmaceutical Chemistry ◽  
Urgent Task ◽  
Methods Of Synthesis ◽  
Pyridine Carboxylic ◽  
Heterocyclic Derivatives ◽  
Synthetic Approaches ◽  
Derivatives Of

The urgent task of modern pharmaceutical chemistry is the development of new methods of synthesis, the study of chemical properties, as well as the search for biologically active compounds among derivatives of nicotinic and isonicotinic acids. The review examines synthetic approaches to the production of carboxylic acid esters including nicotinic and isonicotinic acids, gives examples of the biological activity of nicotinic and isonicotinic acids and their derivatives. The methods for the synthesis of azomethines, substituted acridines and pyrazolones are discussed, examples of their biological activity are given. A promising concept for the synthesis of new potential drugs based on heterocyclic derivatives of nicotinic and isonicotinic acids is presented. The methods of functionalization of organic compounds considered in this review with regard to the synthesis of heterocyclic derivatives of nicotinic and isonicotinic acids make it possible to obtain new promising compounds potentially having antibacterial, antiviral, fungicidal and antitumor activity.

SOME DIRECTIONS IN THE MODIFICATION OF AZOLES

2020 ◽  
Vol 5 (443) ◽  
pp. 85-91
Author(s):  
Ibrayev M.K., ◽  
◽  
Takibayeva A.T., ◽  
Fazylov S.D., ◽  
Rakhimberlinova Zh.B., ◽  
...  
Keyword(s):  
13C Nmr Spectroscopy ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Synthesis Conditions ◽  
Alkaloid Cytisine ◽  
Azole Ring ◽  
Cyclic Compounds ◽  
New Compounds ◽  
Derivatives Of

This article presents studies on the targeted search for new derivatives of azoles, such as benzthiazole, 3,5-dimethylpyrazole, 1,3,4-oxadiazole-2-thione, 1,3,4-thiadiazole. The possibility of combining in one molecule of the azole ring with other cyclic compounds: the alkaloid cytisine, morpholine, furan and some arenes has been studied. To obtain new compounds, the reactions of bromination, acylation, and interaction with isothiocyanates were studied. Optimal synthesis conditions were studied for all reactions. It was found that the reaction of 4-bromo-3,5-dimethylpyrazole with isothiocyanates, in contrast to the previously written derivatives of anilines, takes a longer time and requires heating the reaction mixture. The combination of a pirasol fragment with halide substituents often results in an enhanced therapeutic effect. The synthesized 2-bromine-N-(6-rodanbenzo[d]thiazole-2-yl)acetamide, due to the alkylbromide group, is an important synth in the synthesis of new benzthiazole derivatives. Its derivatives combine in one molecule the rest of rhodanbenzthiazole with alkaloid cytisine and biogenic amine morpholine and are potentially biologically active compounds, since the molecule structure contains several pharmacophoric fragments: benzthiazole and alkaloid (amine) heterocycles, rhodane and urea groups. The mechanism of formation of 1,3,4-oxadiazole-2-tyons from hydrazides under action on them by carbon disulfide was studied and assumed. It was shown that dithiocarbamates in acidic medium decompose with the release of hydrogen sulfide and the formation of highly reactive isothiocyanate group. Then, intra-molecular cyclization occurs, with the formation of end products - 1,3,4-oxadiazole-2-thions. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy. All synthesized substances are potentially biologically active compounds, since they contain several pharmacophore fragments in their structure.

scholarly journals GC-MS Assisted Phytoactive Chemical Compounds Identification and Profiling with Mineral Constituents from Biologically Active Extracts of Aerva javanica (Burm. f) Juss. ex Schult.

2018 ◽  
Vol 46 (2) ◽  
pp. 517-524
Author(s):  
Kandhan KARTHISHWARAN ◽  
Subban KAMALRAJ ◽  
Chelliah JAYABASKARAN ◽  
Shyam S. KURUP ◽  
Sabitha SAKKIR ◽  
...  
Keyword(s):  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Biologically Active ◽  
Scavenging Activity ◽  
Medicinal Uses ◽  
Chemical Structures ◽  
Aerial Parts ◽  
Mineral Constituents

Aerva javanica (Burm. f) Juss. ex Schult. (Family: Amaranthaceae) family is one of the traditional medicinal plant growing in the United Arab Emirates. Apart from studies related to some medicinal properties, phytochemical, GC MS compound characterization and biological activities still to be investigated. An experiment was conducted to determine the possible bioactive components with their chemical structures and elucidation of phytochemicals from the aerial parts of the plant. The macro and micro-mineral constituents and antioxidant activities were also evaluated. Aerial parts of A. javanica were extracted sequentially with hexane, chloroform, ethyl acetate, acetone, methanol by cold percolation method. Free radical scavenging and antioxidant properties of methanolic extract were evaluated by using in vitro antioxidant assays such as hydroxyl radical scavenging activity, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals, superoxide radical scavenging activity and ABTS radical scavenging activity. Primary phytochemical and micro-macro element was tested using standard protocol. The chemical characterization was done with the help of Gas Chromatography-Mass Spectrometry (GC–MS), and the mass spectra of the total compounds in the extract were matched with the National Institute of Standard and Technology (NIST) library. Mineral constituents were identified and estimated by ICP-OES. Ninety-nine metabolites were obtained by GC-MS anslysis; indole was found to be major components followed by 2-Chlorallyl diethyldithiocarbamate (CDEC), Carbaril, Bis(2-ethylhexyl) phthalate, Quinoline, 4H-Cyclopenta[def]phenanthrene,2-[Bis(2-chloroethylamino)]-tetrahydro-2H-1,3,2-oxazaphosphorine-2-oxide, Phenobarbital, 1H-Indole, 2-methyl-, 2,3,7,8-Tetrachlorodibenzo-p-dioxin Disulfide, diphenyl. The presence of various bioactive compounds in the extract validates the traditional medicinal uses of this plant.

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.

Honey as a marinade component for meat semi-finished products

2021 ◽  
Vol 12 (2) ◽  
Author(s):  
L Tyshchenko ◽  
◽  
O Pylypchuk ◽  
V Israelyan ◽  
L Adamchuk ◽  
...  
Keyword(s):  
New Product Development ◽  
New Technologies ◽  
Ph Value ◽  
Current Trend ◽  
Antioxidant Properties ◽  
Meat Products ◽  
Biologically Active ◽  
High Biological Activity ◽  
Water Binding ◽  
Raw Meat

The features of biochemical composition and properties of meat raw materials determine the need to find new technologies for its processing in order to obtain new products with high consumer properties. The current trend in the development of technology is the enrichment of raw meat materials with useful components with functional and technological properties that have a high biological value: apiproducts and products of plant origin. Due to its chemical composition, honey contains about 500 different biologically active substances, which are feasible to use as natural antioxidants in the production of semi-finished meat products. Different types of honey are characterized by high biological activity, dietary and medicinal properties. During heat treatment, meat marinated with honey marinade acquires new taste qualities, the appearance becomes brighter due to the caramelization of honey. The article presents the results of an investigation of the initial raw meat materials, honey, and marinated semi-finished product. We found that a decrease in the pH value of the marinated semi-finished product during a 24-hour treatment period provides meat stability to storage, since most bacteria grow at high pH values, while their growth slows down in acidic nutrient media with pH value below 6.2. Long-term marination makes it possible to obtain meat with increased water-binding and water-holding capacity and improved consistency and juiciness. The task of new product development requires new approaches and techniques in technology. The use of apiproducts, which have antioxidant properties, will allow avoiding the use of food preservatives and stabilizers of chemical origin. Therefore, honey can be used as a part of marinated meat products. The introduction of the active components of honey into the marinade will extend the shelf life and correct the organoleptic properties.

scholarly journals Antioxidant and phytochemical activities of Amaranthus caudatus L. harvested from different soils at various growth stages

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Muhali Olaide Jimoh ◽  
Anthony Jide Afolayan ◽  
Francis Bayo Lewu
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Clayey Loam ◽  
Soil Types ◽  
Growth Stages ◽  
Silty Clay ◽  
Clay Loam ◽  
Amaranthus Caudatus ◽  
Different Soils

Abstract This study aimed at profiling the biological activities of Amaranthus caudatus cultivated on different soils in a glasshouse experiment. Five soil types namely; sandy clay loam, silty clay loam, clayey loam, loam and control (unfractionated soil) were experimentally formulated from primary particles of clay, sand and silt following the United State Department of Agriculture’s (USDA) soil triangle technique. After harvesting at pre-flowering (61 days after planting), flowering (71 days after planting) and post-flowering (91 days after planting) stages, crude extracts were obtained with water and ethanol. Total flavonoids, phenolic and proanthocyanidin contents of the extracts, as well as their biological activities, were determined using 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), 2,2 diphenyl-1-picrylhydrazyl ethanol (DPPH), nitric oxide and phosphomolybdate assays. It was observed that biological activity of A. caudatus varied with soil types, stages of maturity and solvents of extraction. The highest phytochemical yield was recorded in ethanolic extracts of clayey loam harvested prior to flowering and the same trend was replicated in the antioxidant properties of the plant. For optimal biological activity, it is recommended that clayey loam soil should be used for cultivation of A. caudatus and harvest should be made near flowering to capture high phytochemical yield from the species.

scholarly journals Insight into the Presence of Stilbenes in Medicinal Plants Traditionally Used in Croatian Folk Medicine

2016 ◽  
Vol 11 (6) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Ivana Generalić Mekinić ◽  
Danijela Skroza ◽  
Ivica Ljubenkov ◽  
Višnja Katalinić
Keyword(s):  
Biological Activity ◽  
Medicinal Plants ◽  
Biological Activities ◽  
Folk Medicine ◽  
Free Form ◽  
Naturally Occurring ◽  
Derivatives Of ◽  
Insight Into ◽  
Phenolic Extracts

Over the last years, great interest has arisen concerning plant stilbenes, especially resveratrol, which has a whole spectrum of positive biological activities. In this study, we investigated the presence of resveratrol monomers (trans- and cis- form) and naturally occurring derivatives of fraas-resveratrol (piceid, astringin and isorhapontin) in phenolic extracts of twenty medicinal plants traditionally used in Croatian folk medicine. The investigated compounds were present in the samples, in free form or as glucosides, and the highest share was found in immortelle, common yarrow and Lamiaceae plants. The obtained results indicate that biological activity of selected medicinal plants can be related to the presence of this valuable group of phytochemicals.

scholarly journals A REVIEW ON THE SYNTHETIC METHODOLOGIES OF CHROMONES

2018 ◽  
Vol 11 (12) ◽  
pp. 9 ◽  
Author(s):  
Mahathy Vanguru ◽  
Ramchander Merugu ◽  
Swetha Garimella ◽  
Laxminarayana E
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
Biological Applications ◽  
Essential Component ◽  
Wide Range ◽  
Synthetic Methodologies ◽  
New Compounds

Chromones group of compounds and their derivatives form the essential component of pharmacophores in many biologically active molecules. They exhibit a wide range of biological activities such as antibiotic, antitumor, antiviral, antioxidant, antipsychotic, and antihypoxic activities. These applications have stimulated a continuous search for the synthesis of new compounds in this field and are being extensively investigated. The various methodologies so far reported for the synthesis of these compounds with the compounds biological applications are discussed in this communication

Effect of the sulfur-containing compounds on the quinoid process of adrenaline autoxidation; potential neuroprotectors

2019 ◽  
Vol 65 (4) ◽  
pp. 316-323
Author(s):  
T.V. Sirota
Keyword(s):  
Antioxidant Properties ◽  
Enzymatic Reaction ◽  
The Body ◽  
Biologically Active ◽  
Treatment And Prevention ◽  
Multistep Process ◽  
Ic50 Values ◽  
Sulfur Containing ◽  
Sulfur Containing Compounds

The superoxide-generating reaction of adrenaline autoxidation in an alkaline medium, used in vitro to identify the antioxidant properties of various compounds, simulates the complex multistep process of quinoid oxidation of catecholamines (CA) in the body. Sulfur-containing cysteine (Cys) and reduced glutathione (GSH), as well as oxidized glutathione (GSSG), have been shown to inhibit this process. The studied substances were considered as inhibitors of quinoid oxidation and are evaluated as antioxidants. The IC50 values for Cys and GSH were close to 7.5 mM. Inhibition by GSSG was weaker; represented approximately 50-70% of Cys and GSH. Other sulfur-containing compounds that differ in chemical structure, the amino acids taurine and methionine were ineffective. The interest in this model and the search for effective compounds acting on this reaction is associated with one of the mechanisms of the etiopathogenesis of Parkinson's disease (PD) discussed in the literature, which occurs when the biochemical transformations of dopamine CA and its quinoid oxidation process are violated. Cys, GSH and GSSG in the model system inhibit quinoid oxidation of adrenaline, as a result of which the formation of superoxide (O2 ·-) is also inhibited. Experiments with the superoxide-generating enzymatic reaction xanthine xanthioxidase, the chemistry of which is different and not related to formation of quinoid metabolites, showed that the studied substances did not inhibit O2 ·- formation in this model. Thus, it was established that the biologically active sulfur-containing compounds Cys, GSH and GSSG are specific inhibitors of quinoid oxidation of CA, and are likely to be able to play the role of a neuroprotector. It is proposed to use these compounds in the treatment and prevention of PD by activating their biosynthesis in the body.

Sign in / Sign up

Export Citation Format

Share Document