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.

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 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 Synthetic Chiral Derivatives of Xanthones: Biological Activities and Enantioselectivity Studies

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 791 ◽  
Author(s):  
Carla Fernandes ◽  
Maria Carraro ◽  
João Ribeiro ◽  
Joana Araújo ◽  
Maria Tiritan ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Pharmacological Activities ◽  
Sar Studies ◽  
Naturally Occurring ◽  
Structure Activity ◽  
Wide Range ◽  
Synthetic Methodologies ◽  
Derivatives Of ◽  
Biological And Pharmacological Activities

Many naturally occurring xanthones are chiral and present a wide range of biological and pharmacological activities. Some of them have been exhaustively studied and subsequently, obtained by synthesis. In order to obtain libraries of compounds for structure activity relationship (SAR) studies as well as to improve the biological activity, new bioactive analogues and derivatives inspired in natural prototypes were synthetized. Bioactive natural xanthones compromise a large structural multiplicity of compounds, including a diversity of chiral derivatives. Thus, recently an exponential interest in synthetic chiral derivatives of xanthones (CDXs) has been witnessed. The synthetic methodologies can afford structures that otherwise could not be reached within the natural products for biological activity and SAR studies. Another reason that justifies this trend is that both enantiomers can be obtained by using appropriate synthetic pathways, allowing the possibility to perform enantioselectivity studies. In this work, a literature review of synthetic CDXs is presented. The structures, the approaches used for their synthesis and the biological activities are described, emphasizing the enantioselectivity studies.

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.

scholarly journals Synthesis, Acaricidal, Bacteriostatic Activity Among the Amino Derivatives 5,7-Dichloro-4,6-Dinitrobenzofuroxana

2019 ◽  
Vol 8 (2) ◽  
pp. 11-15
Author(s):  
L. V. Spatlova
Keyword(s):  
Biological Activity ◽  
Amino Derivative ◽  
Bacteriostatic Activity ◽  
Hazard Class ◽  
Reaction Conditions ◽  
Low Concentrations ◽  
Wide Range ◽  
Amino Derivatives ◽  
New Compounds ◽  
Derivatives Of

Introduction. In recent years, interest in the compounds of the benzofuroxane series has increased, because they have a wide range of biological activity, and in addition are donors of nitric oxide. In the scientific literature, many works are related to the synthesis and study of the biological activity of 5-nitro-4,6-dichlorobenzofuroxane amino derivatives, whereas amino derivatives of the 5,7-dichlor-4,6-dinitrobenzofuroxane substrate have been poorly studied.Aim. Is the synthesis of new amino derivatives of 5,7-dichloro-4,6-dinitrobenzofuroxane and the study of their biological activity.Materials and methods. Investigated the reaction of condensation of 5,7-dichloro-4,6-dinitrobenzofuroxane with different aromatic amines, containing functional groups of acceptor character in their structure were selected. In order to increase the yield for each specific reaction, the reaction conditions were selected (the reaction temperature, medium, and the amount of amine). The structure of the compounds confirmed IR, NMR spectra and elemental analysis.Results and discussion. New compounds in the 5,7-diamino-4,6-dinitrobenzofuroxane series were obtained. Acute toxicity, acaricidal and bacteriostatic activity against Escherichia coli and Staphylococcus aureus were studied. The obtained compounds were found to have high pharmacological activity, superior to the comparison drug (Chlorophos and Creolin).Conclusion. Most of the amino derivative synthesized 5,7-dichloro-4,6-dinitrobenzofuroxane have a high activity against mites and bacteria. Compounds containing in their structure chlorine and methyl radicals, have biological activity at low concentrations, are low-toxic and belong to the 4th hazard class.

Oximes of Nucleosides and Related Compounds: Synthesis, Reactions and Biological Activity

2018 ◽  
Vol 15 (5) ◽  
pp. 650-665
Author(s):  
Edgars Abele ◽  
Ramona Abele
Keyword(s):  
Biological Activity ◽  
Point Of View ◽  
Nitroso Compounds ◽  
15N Nmr ◽  
Wide Range ◽  
15N Nmr Spectroscopy ◽  
Oxime Derivatives ◽  
Nitrogenous Base ◽  
Synthesis Reactions ◽  
Derivatives Of

Background: Literature data on the synthesis and structure of oximes of nucleosides and related nitrogenous bases from pyrimidine and purine were reviewed. Synthesis of novel heterocyclic systems from nucleoside oximes related pyrimidine oximes was described. The biological activity of derivatives of nucleoside and nitrogenous base oximes was also reviewed. <p> Objective: The review focuses on the recent progress in the area of nucleoside oxime synthesis, reactions and biological activity. Conclusion: In summary, literature data on the synthesis and structure of oximes of nucleosides and related nitrogenous bases derived from pyrimidine, which play an important role in the biological processes, were reviewed. Synthesis of novel heterocyclic systems from nucleoside oximes related pyrimidine oximes was described. The biological activity of derivatives of nucleoside and nucleotide oximes was also reviewed. The studied class of compounds show a wide range of imino-amino and imino-nitroso tautomerism, which was investigated in the presented literature by 1H, 13C and 15N NMR spectroscopy methods. Also, according to the authors point of view, due to imino-amino and/or imino-nitroso tautomerism the nucleoside oximes show interesting activity. Most of the compounds exhibit biological activity characteristic of not only oxime derivatives, but also activity of hydroxylamines or nitroso compounds.

scholarly journals Nanoparticle elasticity regulates phagocytosis and cancer cell uptake

2020 ◽  
Vol 6 (16) ◽  
pp. eaaz4316 ◽  
Author(s):  
Yue Hui ◽  
Xin Yi ◽  
David Wibowo ◽  
Guangze Yang ◽  
Anton P. J. Middelberg ◽  
...  
Keyword(s):  
Cancer Cell ◽  
Cell Uptake ◽  
Receptor Interaction ◽  
Transmission Electron ◽  
Nanoparticle Interactions ◽  
Wide Range ◽  
The Impact ◽  
Specific Ligand ◽  
Silica Nanocapsules

The ability of cells to sense external mechanical cues is essential for their adaptation to the surrounding microenvironment. However, how nanoparticle mechanical properties affect cell-nanoparticle interactions remains largely unknown. Here, we synthesized a library of silica nanocapsules (SNCs) with a wide range of elasticity (Young’s modulus ranging from 560 kPa to 1.18 GPa), demonstrating the impact of SNC elasticity on SNC interactions with cells. Transmission electron microscopy revealed that the stiff SNCs remained spherical during cellular uptake. The soft SNCs, however, were deformed by forces originating from the specific ligand-receptor interaction and membrane wrapping, which reduced their cellular binding and endocytosis rate. This work demonstrates the crucial role of the elasticity of nanoparticles in modulating their macrophage uptake and receptor-mediated cancer cell uptake, which may shed light on the design of drug delivery vectors with higher efficiency.

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.

THE IMPACT OF LEADERSHIP PRACTICES TO TEAM MEMBERS’ SATISFACTION

2009 ◽  
Vol 8 (1) ◽  
Author(s):  
Chalimah .
Keyword(s):  
Conflict Resolution ◽  
Leadership Practices ◽  
Hotel Industry ◽  
Leader Behavior ◽  
Team Leader ◽  
Shop Floor ◽  
Team Members ◽  
Top Executives ◽  
Wide Range ◽  
The Impact

eamwork is becoming increasingly important to wide range of operations. It applies to all levels of the company. It is just as important for top executives as it is to middle management, supervisors and shop floor workers. Poor teamwork at any level or between levels can seriously damage organizational effectiveness. The focus of this paper was therefore to examine whether leadership practices consist of team leader behavior, conflict resolution style and openness in communication significantly influenced the team member’s satisfaction in hotel industry. Result indicates that team leader behavior and the conflict resolution style significantly influenced team member satisfaction. It was surprising that openness in communication did not affect significantly to the team members’ satisfaction.

Stress, anxiety, depression and burnout in frontline health care workers during COVID-19 pandemic: a brief systematic review and new data from Russia

2021 ◽  
Author(s):  
Ekaterina Mosolova ◽  
Dmitry Sosin ◽  
Sergey Mosolov
Keyword(s):  
Risk Factors ◽  
Systematic Review ◽  
Female Gender ◽  
Assessment Tools ◽  
Care Workers ◽  
Younger Age ◽  
Wide Range ◽  
Associated Risk Factors ◽  
Anxiety Depression ◽  
The Impact

During the COVID-19 pandemic, healthcare workers (HCWs) have been subject to increased workload while also exposed to many psychosocial stressors. In a systematic review we analyze the impact that the pandemic has had on HCWs mental state and associated risk factors. Most studies reported high levels of depression and anxiety among HCWs worldwide, however, due to a wide range of assessment tools, cut-off scores, and number of frontline participants in the studies, results were difficult to compare. Our study is based on two online surveys of 2195 HCWs from different regions of Russia during spring and autumn epidemic outbreaks revealed the rates of anxiety, stress, depression, emotional exhaustion and depersonalization and perceived stress as 32.3%, 31.1%, 45.5%, 74.2%, 37.7% ,67.8%, respectively. Moreover, 2.4% of HCWs reported suicidal thoughts. The most common risk factors include: female gender, nurse as an occupation, younger age, working for over 6 months, chronic diseases, smoking, high working demands, lack of personal protective equipment, low salary, lack of social support, isolation from families, the fear of relatives getting infected. These results demonstrate the need for urgent supportive programs for HCWs fighting COVID-19 that fall into higher risk factors groups.

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