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.

scholarly journals RETENTION BEHAVIOR AND BIOLOGICAL ACTIVITY OF N-SUBSTITUTED-2-PHENYLACETAMIDE DERIVATES

2014 ◽  
Vol 5 (1) ◽  
Author(s):  
Đenđi Vaštag ◽  
Suzana Apostolov ◽  
Borko Matijević ◽  
Jelena Nakomčić ◽  
Aleksandar Marinković
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Biological Properties ◽  
Reversed Phase ◽  
Chromatographic Retention ◽  
Wide Range ◽  
Structure Retention ◽  
The Mathematical Model ◽  
The Relationship ◽  
Layer Chromatography

Phenylacetamide derivatives are a group of compounds that exhibit a wide range of biological activities as analgetic, anticonvulsant, pesticide, cytostatic. It is well known that the biological activity and the field of activity of the substance are greatly dependent on its physical, chemical and structural properties. In this paper, we applied QSRR analysis (Quantitative Structure Retention Relationships), which is based on the prediction of biological properties of compounds based on their chromatographic retention behaviors. To that end, retention constants of investigated N-substituted-2-phenylacetamide were determined by reversed phase thin-layer chromatography, (HPTLC RP18 F254s) in the presence of different volume fractions of n-propanol and tetrahydrofuran. The resulting data were correlated with molecular descriptors determined in different ways in order to establish the mathematical model that describes the relationship between retention properties and biological activities of investigated phenylacetamides.

Biological Function and Chemistry of Endothelin. A Review

1999 ◽  
Vol 64 (8) ◽  
pp. 1211-1252 ◽  
Author(s):  
Jan Hlaváček ◽  
Renáta Marcová
Keyword(s):  
Biological Activity ◽  
Amino Acid ◽  
Biological Function ◽  
Biological Properties ◽  
Structural Basis ◽  
Amino Acid Residues ◽  
Snake Venoms ◽  
Vasoactive Peptides ◽  
Physico Chemical ◽  
Endothelin A

The first part of this review deals with the biosynthesis and a biological function of strongly vasoactive peptides named endothelins (ETs) including vasoactive intestinal contractor. Where it was useful, snake venoms sarafotoxins which are structural endothelin derivatives, were also mentioned. In the second part, an attention is paid to structural basis of the ETs biological activity, with respect to alterations of amino acid residues in the parent peptides modifying the conformation and consequently the physico-chemical and biological properties in corresponding ETs analogs. Special attention is focussed on the area of ETs receptors and their interaction with peptide and non peptide agonists and antagonists, important in designing selective inhibitors of ETs receptors potentially applicable as drugs in a medicine. A review with 182 references.

scholarly journals Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
High Reactivity ◽  
Biologically Active ◽  
Brain Lipids ◽  
Wide Range ◽  
Privileged Structure ◽  
Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

Effects of pollution and climate change on the ecosystem components

2021 ◽  
Author(s):  
Yuriy Lykholat
Keyword(s):  
Endocrine System ◽  
Biologically Active ◽  
Soil Conditions ◽  
Negative Effects ◽  
Current State ◽  
Herbaceous Communities ◽  
Active Chemical ◽  
Study Results ◽  
Ecological Patterns ◽  
The Relationship

The book contains the study results of the environmental and soil conditions of the transformed territories, the ecological patterns of woody plants natural communities’ formation as well as the features of the herbaceous communities’ succession in flooded areas. The current state of forest areas is highlighted, the problems of forest management and their exploitation in Ukraine are outlined. Aspects of anthropogenic impact on natural aquatic ecosystems are shown and various biotesting methods of negative effects are characterized. The relationship between the presence of exogenous biologically active chemical compounds in the environment and damage to the endocrine system of animals has been revealed. The scientific manuscript is intended for ecologists, specialists interested in environmental management and environmental protection. The book may be useful for graduate students and scientific researchers.

scholarly journals Inositol phosphates: health implications, methods of analysis, and occurrence in plant foods

2018 ◽  
Vol 1 ◽  
Author(s):  
Quynh H. Duong ◽  
Karen G. Lapsley ◽  
Ronald B. Pegg
Keyword(s):  
Inositol Phosphates ◽  
Negative Effects ◽  
Plant Foods ◽  
Plant Seeds ◽  
Cell Functions ◽  
Wide Range ◽  
Multiple Cell ◽  
The Relationship

Inositol phosphates (InsPs), especially myo-inositol hexakisphosphate (InsP6), are important binders of phosphorus and minerals in plant seeds. However, they have long been considered as anti-nutritional components of plant foods due to their possible negative effects on the absorption of minerals and proteins in mammals. On the other hand, recent findings have found InsPs to be ubiquitous in eukaryote cells and actively participating in multiple cell functions. In vivo and in vitro studies have also documented the preventive potential of these compounds against the development of a wide range of diseases. In light of these findings, interest in the relationship between these compounds and human health has been renewed. It is suggested that the interactions of InsPs with other nutrients in the gut are complex, that the absorption of dietary InsPs might be implied but is not certain, and that the disease fighting capabilities of InsPs hold both promises and limitations. At the same time, the analysis of these compounds in foods and biological samples still faces many challenges, calling for more advanced modification and developments in the future.

scholarly journals Secondary metabolites of a marine-derived Penicillium ochrochloron

2021 ◽  
Vol 13 (3) ◽  
pp. 11020
Author(s):  
Peter M. EZE ◽  
Ying GAO ◽  
Yang LIU ◽  
Lasse Van GEELEN ◽  
Chika P. EJIKEUGWU ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Secondary Metabolites ◽  
Biological Properties ◽  
Industrial Applications ◽  
Biologically Active ◽  
Fungal Isolation ◽  
The North ◽  
Wide Range ◽  
Extremophilic Fungi ◽  
Fungal Secondary Metabolites

Extremophilic fungi have received considerable attention recently as new promising sources of biologically active compounds with potential pharmaceutical applications. This study investigated the secondary metabolites of a marine-derived Penicillium ochrochloron isolated from underwater sea sand collected from the North Sea in St. Peter-Ording, Germany. Standard techniques were used for fungal isolation, taxonomic identification, fermentation, extraction, and isolation of fungal secondary metabolites. Chromatographic separation and spectroscopic analyses of the fungal secondary metabolites yielded eight compounds: talumarin A (1), aspergillumarin A (2), andrastin A (3), clavatol (4), 3-acetylphenol (5), methyl 2,5-dihydro-4-hydroxy-5-oxo-3-phenyl-2-furanpropanoate (6), emodin (7) and 2-chloroemodin (8). After co-cultivation with Bacillus subtilis, the fungus was induced to express (-)-striatisporolide A (9). Compound 1 was evaluated for antibacterial activity against Staphylococcus aureus, Acinetobacter baumannii, Mycobacterium smegmatis, and M. tuberculosis, as well as cytotoxicity against THP-1 cells. The compound, however, was not cytotoxic to THP-1 cells and had no antibacterial activity against the microorganisms tested. The compounds isolated from P. ochrochloron in this study are well-known compounds with a wide range of beneficial biological properties that can be explored for pharmaceutical, agricultural, or industrial applications. This study highlights the bioprospecting potential of marine fungi and confirms co-cultivation as a useful strategy for the discovery of new natural products.

scholarly journals The action of potassium and other ions on the injury potential and action current in maia nerve

1934 ◽  
Vol 115 (793) ◽  
pp. 216-260 ◽  
Keyword(s):  
Electrolyte Solutions ◽  
Ion Concentration ◽  
Action Current ◽  
A Value ◽  
Physico Chemical ◽  
Wide Range ◽  
The Difference ◽  
Living Tissues ◽  
The Relationship ◽  
Injury Potential

The electric currents in living tissues have interested physiologists ever since their existence was proved by Du Bois Reymond, but little was done towards explaining their origin and magnitude on a quantitative physico-chemical basis befor the pioneer researches og J. S. Macdonald. Work previous to Macdonald's has discussed fully by that anuthor (1902), hence it will not be mentioned here. macdonald found that the injury potential of medullated nerve, either frog's or mammal's (1900, a, b ; 1902), could be given a value greater or smaller than the normal by simply altering the concentration of the solution in contact with the external surfaces of the fibres. He showed that solutions of NaOH, HCl, NaCl, or KCl affected the potential according to their concentrations and that the relationship between the two variables was a logarithmic one, which fact was in agreement with the then new theory of concentration cells developed by Nernst. Macdonald went on to point out (1902) that the effects of potassium chloride solutions were particularly interesting, and to suggest that the difference between the concentration of potassium in the axis cylinder of the nerve and in the surrounding blood or salt solution was wholly responsible for the observed injury potential. Over a wide range of concentration, 1/8 to 1 molar, he demonstrated that there was nearly a linear relation between the injury potential and the logarithm of the potassium ion concentration. However, since he simply varied the concentrations of his electrolyte solutions, and made no effort to maintain them isotonic with blood by the addition of a non-electrolyte, exception might be taken to some of his results on the ground that the effects were due in part to the passage of water into or out of the nerve with a consequent dilution or concentration of the plasma.

scholarly journals Preparation of polyclonal and monoclonal anti-idiotypic antibodies against morphine-specific immunoglobulins

2020 ◽  
Vol 22 (1) ◽  
pp. 187-196
Author(s):  
A. V. Trofimov ◽  
V. A. Atanesyan ◽  
A. M. Ischenko ◽  
E. A. Karabanova ◽  
A. Ya. Rak ◽  
...  
Keyword(s):  
First Generation ◽  
Polyclonal Antibodies ◽  
Practical Importance ◽  
Biologically Active ◽  
Animal Blood ◽  
Physico Chemical ◽  
Antigenic Properties ◽  
Wide Range ◽  
Secondary Antibodies ◽  
Mouse Myeloma

The preparation and study of anti-idiotypic (secondary) antibodies (Ab2) against monoclonal primary antibodies (Ab1) specific to biologically active molecules with a known structure is of great scientific and practical importance. Due to partial antigenic similarity of Ab2 and the initial antigen structures, these antibodies can be the basis of the vaccine, if the antigen usage is not possible, or is limited by law. In particular, one may create Ab2-based preparations, designed for immunization, in order to prevent and treat the drug addiction. The value of Ab2 properties increases even more if Ab1, used to obtain them, recognize different parts of the antigen molecule, which makes it possible to obtain second-generation antibodies with a wide range of specificity. In this work, the morphine-like polyclonal and monoclonal Ab2 were obtained. In each case, as the first-generation immunoglobulins for immunization, we used two murine monoclonal antibodies (mAbs) specific to different morphine derivatives: 3K11 antibodies to 3-0-carboxymethyl (CMM) and 2-p-carboxyphenylazomethyl (FAM) derivatives, as well as 6G1 antibodies to 6-hemisuccinyl derivative (GSM). After immunization of the horse with Ab1 and development of immune response, three pools of specific polyclonal antibodies were isolated from the animal blood serum: horse anti-species antibodies to the total mouse immunoglobulins (HAM); horse anti-idiotypic antibodies against 3K11 antibodies (HAM-K11), and against 6G1 antibodies (HAM-G1). In parallel, immunization of mice with 3K11 and 6G1 antibodies and fusion of obtained lymphocytes with Sp2/0 mouse myeloma cells by the Milstein-Köhler method resulted in three producers of anti-idiotypic antibodies: a clone producing mouse monoclonal Ab2 specific for mAb-6G1 (AIG1), as well as clones producing anti-mAb-3K11 antibodies (AI-K11A and AI-K11B). The physico-chemical and antigenic properties of all the Ab2 obtained were characterized. It was shown that the horse anti-idiotypic immunoglobulins not only belong to different classes, but are also polyvalent, while all monoclonal Ab2 obtained are represented by IgM immunoglobulins, being also strictly specific to the corresponding first-generation antibodies. Subsequently, the morphine-like properties of the first domestic polyclonal and monoclonal Ab2 obtained in the work will be investigated in a cellular model. Likewise, we shall study their ability to induce Ab3 as well as morphine-specific Ab1.

Metal Ion Complexes with Pyrazoles, Aziridines and Diaziridines – Synthesis and Biological Activity

2019 ◽  
Vol 26 (4) ◽  
pp. 648-663 ◽  
Author(s):  
Katarzyna Malinowska ◽  
Ingo-Peter Lorenz ◽  
Beata Sadowska ◽  
Paulina Mucha
Keyword(s):  
Biological Activity ◽  
Metal Ion ◽  
Biological Significance ◽  
Antimicrobial Properties ◽  
Transition Metal Ions ◽  
Antitumor Action ◽  
Metal Ion Complexes ◽  
Current State ◽  
Wide Range ◽  
The Relationship

Heterocyclic compounds containing nitrogen ions, like pyrazoles, aziridines, diaziridines and their metal ion complexes with Cu(II), Zn(II) and Ru(III) and others exhibit a wide range of biological activity, including mainly anti-inflammatory, antioxidant, anticancer, and antimicrobial properties. Biological significance of these molecules and thus their potential use in medicine has driven growing interest into their coordination chemistry. A knowledge of the relationship between the structure of chemical compounds and their activity is needed for the synthesis of the preparations possessing the most beneficial features. The choice of interposed substituents may improve biocidal and antitumor action, reduce the toxicity of the initial substance, or even completely eliminate its adverse effects for healthy tissues. The main aim of this review paper is to present the current state of knowledge concerning the synthesis and biological activity of complexes with small heterocyclic ligands containing transition metal ions.

Syntheses and Biological Activities of triazole-based Sulfonamides

2020 ◽  
Vol 23 (21) ◽  
pp. 2319-2349 ◽  
Author(s):  
Ali Ramazani ◽  
Hamed Sadighian ◽  
Farideh Gouranlou ◽  
Sang W. Joo
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Potential Biological Activity

: The triazole and sulfonamide compounds are known as biologically active agents that were employed for medicinal applications. These compounds were obtained in different forms by a variety of techniques to vast ranges of applications. The broad biological properties of these compounds have encouraged researchers to design and synthesize triazole-based sulfonamide derivatives as compounds with potential biological activity. In this review, we summarized the synthetic procedures of triazole-based sulfonamide compounds together with their biological activities during the last two decades.

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