scholarly journals Predicted screening of biological activity of thiosulphonate pyrimidine derivatives

2020 ◽  
Vol 3 (2) ◽  
pp. 53-60
Author(s):  
N. Ya. Monka ◽  
◽  
N. Ye. Stadnytska ◽  
R. V. Charka ◽  
Y. V. Roman ◽  
...  
Keyword(s):  
Biological Activity ◽  
Experimental Studies ◽  
Biological Action ◽  
New Drugs ◽  
Toxic Substances ◽  
Practical Application ◽  
Pyrimidine Derivatives ◽  
Wide Range ◽  
Depth Study ◽  
On Line

Pyrimidine and its derivatives are important objects for chemical synthesis and development of new drugs based on them. There is a practical application of a number of substances with a pyrimidine heterocycle in medical practice. We performed a predicted screening of biological activity, cytotoxicity and toxicity in rats of some synthesized pyrimidine thiosulfonates using appropriate on-line programs. It was found that they are low-toxic substances with a wide range of biological action and a high value of probable activity, which indicates the feasibility of continuing experimental studies of their biological action, in particular anticancer. S- (4,6- dimethylpyrimidin-2-yl) benzenesulfonothioate deserves special attention for in-depth study.

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.

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 Osipovs’s fire nozzles as a means of combating environmental pollution

2020 ◽  
Vol 193 ◽  
pp. 02004
Author(s):  
Arthur Osipov
Keyword(s):  
Environmental Pollution ◽  
Forest Fires ◽  
Harmful Effect ◽  
Experimental Studies ◽  
Toxic Substances ◽  
Practical Application ◽  
Empirical Formulas ◽  
Full Scale Tests ◽  
Combustible Liquids

The classification of the main types of fires is provided, their effect on environmental pollution and adversely affecting people’s health is noted. The harmful effect of the consequences of forest fires on the ecology is shown, the main toxic substances released into the atmosphere are given. The harm caused by industrial fires of flammable and combustible liquids is analyzed. The specifics of extinguishing these fires and the need for Osipovs’s fire nozzles are substantiated. Design features of Osipovs’s fire nozzles are considered. The basics of calculating their tactical and technical characteristics are given. The effectiveness of their practical application in extinguishing forest and industrial fires of oil products is shown. Analytical studies of literary material were conducted. Calculation according empirical formulas and schemes is provided. Polygon and full-scale tests of Osipovs’s manual and fire monitors are presented. As a result of theoretical and experimental studies, the design was optimized and the tactics of using these fire nozzles in a fire were developed. The practical application of Osipovs’s manual and fire monitors allows get better the working conditions of nozzlemans, increasing fire fighting efficiency, reducing environmental pollution and improving its ecology.

Load Flow Analysis Using Improved Newton-Raphson Method

2015 ◽  
Vol 793 ◽  
pp. 494-499 ◽  
Author(s):  
Chieng Kai Seng ◽  
Tay Lea Tien ◽  
Janardan Nanda ◽  
Syafrudin Masri
Keyword(s):  
Solution Method ◽  
Flow Analysis ◽  
Load Flow ◽  
Practical Application ◽  
Load Flow Analysis ◽  
Wide Range ◽  
The Matrix ◽  
On Line ◽  
Raphson Method ◽  
Computation Speed

This paper describes a simple, reliable and swift load-flow solution method with a wide range of practical application. It is attractive for accurate or approximate off-and on-line calculations for routine and contingency purposes. It is applicable for networks of any size and can be executed effectively on computers. The method is a development on conventional load flow principle and its precise algorithm form has been determined to bring improvement to the conventional techniques. This paper presents a comparative study of the new constant Jacobian matrix load flow method built based on several conventional NR load flow methods. Assumptions are made so as to make the matrix constant, thus eliminating the need of calculating the matrix in every iteration. The proposed method exhibits better computation speed.

scholarly journals Peran Herpetofauna dalam Bidang Kesehatan: Peluang dan Tantangan

2018 ◽  
Vol 4 (1) ◽  
pp. 38-49
Author(s):  
Aditya K. Karim ◽  
Zainal A. Wasaraka ◽  
Linus Y. Chrystomo ◽  
Ervina Indrayani
Keyword(s):  
Biological Activity ◽  
Drug Development ◽  
Human Health ◽  
Mode Of Action ◽  
Antidiabetic Activity ◽  
Practical Application ◽  
Skin Secretion ◽  
Wide Range ◽  
Skin Secretions ◽  
Pharmaceutical Agents

Skin secretions and venom from many species of amphibi (frogs and toads) and reptil (group of herpetofauna) from different famillies contain a wide range of unique physiological compounds with biological activity such as peptide, protein, non-protein, and enzyme. They are potent for drug development. The compounds, known as mode of action have practical application as pharmaceutical agents, diagnostic reagents or preparative tools. Peptides with potential anticancer, fibrinolityc, antibacterial, antifungal, antidiabetic activity play important roles in human health. This review introduces roles of herpetofauna for drugs development, potential therapeutic values and their application in human health and disease.Key words: Herpetofauna, skin secretion, venom, drugs development, health.

Recent Progress and Plans in Computer-Controlled High Resolution Electron Microscopy

1990 ◽  
Vol 48 (1) ◽  
pp. 154-155
Author(s):  
W.J. de Ruijter ◽  
Peter Rez ◽  
David J. Smith
Keyword(s):  
Electron Microscopy ◽  
Digital Processing ◽  
High Resolution Electron Microscopy ◽  
Objective Lens ◽  
Linear Filter ◽  
Contrast Transfer Function ◽  
Image Displacement ◽  
Spatially Resolved ◽  
Wide Range ◽  
On Line

Digital computers are becoming widely recognized as standard accessories for electron microscopy. Due to instrumental innovations the emphasis in digital processing is shifting from off-line manipulation of electron micrographs to on-line image acquisition, analysis and microscope control. An on-line computer leads to better utilization of the instrument and, moreover, the flexibility of software control creates the possibility of a wide range of novel experiments, for example, based on temporal and spatially resolved acquisition of images or microdiffraction patterns. The instrumental resolution in electron microscopy is often restricted by a combination of specimen movement, radiation damage and improper microscope adjustment (where the settings of focus, objective lens stigmatism and especially beam alignment are most critical). We are investigating the possibility of proper microscope alignment based on computer induced tilt of the electron beam. Image details corresponding to specimen spacings larger than ∼20Å are produced mainly through amplitude contrast; an analysis based on geometric optics indicates that beam tilt causes a simple image displacement. Higher resolution detail is characterized by wave propagation through the optical system of the microscope and we find that beam tilt results in a dispersive image displacement, i.e. the displacement varies with spacing. This approach is valid for weak phase objects (such as amorphous thin films), where transfer is simply described by a linear filter (phase contrast transfer function) and for crystalline materials, where imaging is described in terms of dynamical scattering and non-linear imaging theory. In both cases beam tilt introduces image artefacts.

Modern prevention and active longevity programs on the basis of disruptive domestic technologies: positive experience and prospects for application

2020 ◽  
pp. 66-73
Author(s):  
A. Simonova ◽  
S. Chudakov ◽  
R. Gorenkov ◽  
V. Egorov ◽  
A. Gostry ◽  
...  
Keyword(s):  
Personalized Medicine ◽  
Early Detection ◽  
Laboratory Diagnostics ◽  
Positive Experience ◽  
Practical Application ◽  
Wide Range ◽  
Integrated Program ◽  
Long Term Experience ◽  
Early Detection And Prevention

The article summarizes the long-term experience of practical application of domestic breakthrough technologies of preventive personalized medicine for laboratory diagnostics of a wide range of socially significant non-infectious diseases. Conceptual approaches to the formation of an integrated program for early detection and prevention of civilization diseases based on these technologies are given. A vision of the prospects for the development of this area in domestic and foreign medicine has been formed.

Generic monitoring tools for water characteristics assessment

2003 ◽  
Vol 3 (1-2) ◽  
pp. 351-357
Author(s):  
S. Le Bonté ◽  
M.-N. Pons ◽  
O. Potier ◽  
S. Chanel ◽  
M. Baklouti
Keyword(s):  
Municipal Wastewater ◽  
Principal Component ◽  
Toxic Substances ◽  
Capacity Curves ◽  
Water Characteristics ◽  
Monitoring Tools ◽  
Visible Spectra ◽  
On Line ◽  
Mining Procedure

An adaptive principal component analysis applied to sets of data provided by global analytical methods (UV-visible spectra, buffer capacity curves, respirometric tests) is proposed as a generic procedure for on-line and fast characterization of wastewater. The data-mining procedure is able to deal with a large amount of information, takes into account the normal variations of wastewater composition related to human activity, and enables a rapid detection of abnormal situations such as the presence of toxic substances by comparison of the actual wastewater state with a continuously updated reference. The procedure has been validated on municipal wastewater.

Biological Activity of Trans-Membrane Anion Carriers

2018 ◽  
Vol 25 (30) ◽  
pp. 3560-3576 ◽  
Author(s):  
Massimo Tosolini ◽  
Paolo Pengo ◽  
Paolo Tecilla
Keyword(s):  
Biological Activity ◽  
Membrane Transport ◽  
Anticancer Agents ◽  
Biological Effects ◽  
Structure Activity Relationship ◽  
New Drugs ◽  
Activity Relationship ◽  
Anion Channels ◽  
Cellular Homeostasis ◽  
Structure Activity

Natural and synthetic anionophores promote the trans-membrane transport of anions such as chloride and bicarbonate. This process may alter cellular homeostasis with possible effects on internal ions concentration and pH levels triggering several and diverse biological effects. In this article, an overview of the recent results on the study of aniontransporters, mainly acting with a carrier-type mechanism, is given with emphasis on the structure/activity relationship and on their biological activity as antibiotic and anticancer agents and in the development of new drugs for treating conditions derived from dysregulation of natural anion channels.

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