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.

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 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 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 Optimized Synthesis of New Thiosemicarbazide Derivatives with Tuberculostatic Activity

2021 ◽  
Vol 22 (22) ◽  
pp. 12139
Author(s):  
Corina Popovici ◽  
Cristina-Maria Pavel ◽  
Valeriu Sunel ◽  
Corina Cheptea ◽  
Dan Gheorghe Dimitriu ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Spectral Analysis ◽  
Elemental Analysis ◽  
Tuberculostatic Activity ◽  
Medical Applications ◽  
Wide Range ◽  
Biological Tests ◽  
Ft Ir ◽  
Thiosemicarbazide Derivatives

Original results are presented in the field of research that addresses the extension of the reaction of residue of acyl-thiosemicarbazide fixation on the structure of 5-nitrobenzimidazole by a sulphonic group. The aim of the study is the increase of new thiosemicarbazide derivatives’ applicative potential in the field of biochemistry, with a wide range of medical applications. The newly obtained compounds were characterized by using elemental analysis and spectral analysis (FT-IR and 1H NMR). A study regarding the optimization of the chemical reactions was made. The performed in vitro biological tests confirmed the tuberculostatic activity of three newly obtained compounds against Mycobacterium tuberculosis.

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.

Enzymes as a Reservoir of Host Defence Peptides

2020 ◽  
Vol 20 (14) ◽  
pp. 1310-1323
Author(s):  
Andrea Bosso ◽  
Antimo Di Maro ◽  
Valeria Cafaro ◽  
Alberto Di Donato ◽  
Eugenio Notomista ◽  
...  
Keyword(s):  
Innate Immunity ◽  
Biological Activity ◽  
Internal Structure ◽  
Catalytic Properties ◽  
Cellular Responses ◽  
Host Defence ◽  
Present Review ◽  
Active Peptides ◽  
Wide Range

Host defence peptides (HDPs) are powerful modulators of cellular responses to various types of insults caused by pathogen agents. To date, a wide range of HDPs, from species of different kingdoms including bacteria, plant and animal with extreme diversity in structure and biological activity, have been described. Apart from a limited number of peptides ribosomally synthesized, a large number of promising and multifunctional HDPs have been identified within protein precursors, with properties not necessarily related to innate immunity, consolidating the fascinating hypothesis that proteins have a second or even multiple biological mission in the form of one or more bio-active peptides. Among these precursors, enzymes constitute certainly an interesting group, because most of them are mainly globular and characterized by a fine specific internal structure closely related to their catalytic properties and also because they are yet little considered as potential HDP releasing proteins. In this regard, the main aim of the present review is to describe a panel of HDPs, identified in all canonical classes of enzymes, and to provide a detailed description on hydrolases and their corresponding HDPs, as there seems to exist a striking link between these structurally sophisticated catalysts and their high content in cationic and amphipathic cryptic peptides.

Synthesis and Biological Potentials of Quinoline Analogues: A Review of Literature

2019 ◽  
Vol 16 (7) ◽  
pp. 653-688 ◽  
Author(s):  
Leena Kumari ◽  
Salahuddin ◽  
Avijit Mazumder ◽  
Daman Pandey ◽  
Mohammad Shahar Yar ◽  
...  
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Building Blocks ◽  
Vital Role ◽  
Review Of Literature ◽  
Drug Discovery Process ◽  
Active Compounds ◽  
Lead Compounds ◽  
Synthetic Approaches ◽  
Derivatives Of

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

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