scholarly journals Natural Sesquiterpene Lactones as Renewable Chemical Materials for New Medicinal Products

2013 ◽  
Vol 15 (3) ◽  
pp. 163 ◽  
Author(s):  
S.M. Adekenov
Keyword(s):  
Chemical Modification ◽  
Sesquiterpene Lactones ◽  
Physiological Activity ◽  
Chemical Properties ◽  
Water Soluble ◽  
Biologically Active ◽  
Isolation And Purification ◽  
Environmentally Safe ◽  
Renewable Material ◽  
Derivatives Of

<p>Literature data and own research results on the technology for isolating natural sesquiterpene lactones such as arglabin, alantolactone, artemisinin, grosheimin, isoalantolactone, parthenolide, santonin and potential possibilities of their use as renewable material for obtaining new compounds as well as biologically active derivatives are generalized in this review. Sesquiterpene lactones from plants are promising sources for the development and practical application of new original medical products possessing antitumor, anti-inflammatory, antimalarial, antiulcer, antiviral and immune-stimulating action. The technology for isolating sesquiterpene lactones is based on the extraction of raw plant material by different organic solvents with the subsequent chromatographic purification. The effective and environmentally safe technology for isolation and purification of sesquiterpene lactone arglabin from <em>Artemisia glabella</em> Kar. et Kir. by the СО<sub>2</sub>-extraction method is developed. Thereat, it was experimentally determined that the method for isolating arglabin from CO<sub>2</sub> extract of <em>Artemisia glabella</em> Kar. et Kir. using centrifugal partition chromatography is effective for preparative isolation of the active substance and its manufacturing application. It is practically important to obtain water-soluble derivatives of biologically active sesquiterpene lactones and also to use the nanotechnology achievements for directed transportation of a molecule of the medicine in the human body thereby reducing toxicity of an active component. Promising direction is chemical modification of molecules in sesquiterpene lactones which are renewable material for obtaining new derivatives, thanks to which it becomes possible to solve two problems at the same time. Firstly, these researches help to obtain derivatives with higher biological activity or improved physical and chemical properties. Secondly, these researches enable us to disclose the mechanism of action of different medicines within the framework of “structure-activity” correlation. The article presents the literature data and own results on chemical modification of sesquiterpene lactones of alantolactone, arglabin, artemisinin, grosheimin, isoalantolactone, parthenolide and santonin. Various reactions on functional groups of these molecules were used to obtain a number of new derivatives of sesquiterpene lactones containing haloid-, pyrazole-, triazole-, amino-, dialkylamino-, hydroxy-, dialkyl phosphonate- and cyclopropane groups, which have shown high physiological activity.</p>

FULLERENECARBOXYLIC ACIDS AND PROSPECTS FOR THEIR USE IN THE CHEMISTRY OF DRUGS

2018 ◽  
Vol 18 (2) ◽  
pp. 19-28
Author(s):  
E V Litasova ◽  
L B Piotrovskiy
Keyword(s):  
Delivery Systems ◽  
Water Soluble ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Carboxyl Groups ◽  
Derivatives Of ◽  
Active Substances

Among the various derivatives of fullerenes, compounds containing carboxyl groups (carboxyfullerenes) occupy a prominent place. The reason is that the introduction of carboxyl groups makes it possible to obtain water-soluble derivatives of highly lipophilic fullerenes. The review deals with matters of synthesis and structure of carboxyfullerenes, the influence of the amount and structure of the addends on the solubility of the entire compound, various aspects of the usage of these compounds as independent biologically active substances and carriers for creation of various delivery systems.

scholarly journals Influence of Biologically Active Substances on Key Indicators of the Conditions of Winter Wheat Ecocenosis

2021 ◽  
Vol 100 ◽  
pp. 05010
Author(s):  
Oleksandr Zabolotnyi ◽  
Larysa Rozborska ◽  
Iryna Leontiuk ◽  
Ivan Zhilyak ◽  
Anna Datsenko
Keyword(s):  
Plant Growth ◽  
Winter Wheat ◽  
Growth Regulator ◽  
Malonic Dialdehyde ◽  
Water Soluble ◽  
Rhizosphere Bacteria ◽  
Biologically Active ◽  
Environmentally Safe ◽  
High Yields ◽  
Active Substances

The article deals with the study of the effect of the application of the herbicide Granstar Gold 75, w.g. (water-soluble granulate) and plant growth regulator Regoplant on some ecological indicators of ecocenosis of winter wheat sowing (lipid peroxidation reactions in winter wheat plants by the activity of malonic dialdehyde content accumulation, enzymatic activity, total number of rhizosphere bacteria and anatomical structure of winter wheat leaves). The choice of research topic is due to the fact that currently obtaining high yields of winter wheat is closely connected to the widespread use of chemicals, in particular, herbicides, which by their nature are physiologically active substances that can affect both plants and soil microbiota. This, in turn, leads to the search for environmentally safe elements of technologies for growing winter wheat. One such element may be the use of herbicides together with plant growth regulators. The obtained experimental data testify to the protective ability of the growth regulator Regoplant against the winter wheat plants, as evidenced by a decrease in the activity of malonic dialdehyde accumulation, changes in the activity of the enzymatic defense system, decrease the number of epidermis cells and an increase in total rhizosphere bacteria in case of Regoplant use together with Granstar Gold 75, w.g. compared with the experiment variants, where the herbicide was applied without a growth regulator. That is, the use of growth regulator in a mixture with herbicide to some extent eliminates the toxic effect of xenobiotics, which has a positive effect on the state of ecobiosis of winter wheat sowing.

A Facile Synthesis of substituted Trifluoromethyl piperidines with diversify functionalization

2021 ◽  
Vol 18 ◽  
Author(s):  
Wahid Bux Jatoi ◽  
Ashique Hussain Balouch ◽  
Mazhar Iqbal Khaskheli ◽  
Nafeesa Khatoon Shahani ◽  
Qurat-Ul-Ain Shaikh ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Biologically Active ◽  
Physical And Chemical Properties ◽  
Great Tendency ◽  
Facile Synthesis ◽  
Physical And Chemical ◽  
Derivatives Of ◽  
Aromatic Heterocyclic ◽  
Active Natural ◽  
And Chemical Properties

: Piperidine-based alkaloids are undoubtedly an important class of biologically active natural products. When a unique group like trifluoromethyl (Tfm) is added to an active compound, it significantly ameliorates its bioactivity, bioavailability, physical and chemical properties. Many fluorination and trifluoromethylation methods have been reported. In the present paper, we have shown that among all other trifluoromethylation pathways, Mannich reaction also has the great tendency to introduce a Tfm group in a saturated or aromatic heterocyclic compound. Applications of this reaction are elaborated in preparing several derivatives of piperidine base alkaloids with trifluoromethyl at α-position. Furthermore, the substitution at C-4 and C-6 was successfully achieved with variety of saturated and aromatic groups.

Colloid-chemical properties and physiological activity of water-soluble humic preparations

2016 ◽  
Vol 89 (6) ◽  
pp. 969-974
Author(s):  
N. V. Yudina ◽  
E. V. Mal’tseva ◽  
A. S. Smirnova ◽  
E. M. Berezina
Keyword(s):  
Physiological Activity ◽  
Chemical Properties ◽  
Water Soluble

scholarly journals HPMA-Based Polymer Conjugates for Repurposed Drug Mebendazole and Other Imidazole-Based Therapeutics

Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2530
Author(s):  
Martin Studenovský ◽  
Anna Rumlerová ◽  
Libor Kostka ◽  
Tomáš Etrych
Keyword(s):  
Chemical Properties ◽  
Drug Repurposing ◽  
Water Soluble ◽  
Biologically Active ◽  
Lysosomal Hydrolases ◽  
Polymer Carrier ◽  
Design Synthesis ◽  
Polymer Conjugates ◽  
Synthetic Strategy ◽  
Physico Chemical

Recently, the antitumor potential of benzimidazole anthelmintics, such as mebendazole and its analogues, have been reported to have minimal side effects, in addition to their well-known anti-parasitic abilities. However, their administration is strongly limited owing to their extremely poor solubility, which highly depletes their overall bioavailability. This study describes the design, synthesis, and physico-chemical properties of polymer-mebendazole nanomedicines for drug repurposing in cancer therapy. The conjugation of mebendazole to water-soluble and biocompatible polymer carrier was carried out via biodegradable bond, relying on the hydrolytic action of lysosomal hydrolases for mebendazole release inside the tumor cells. Five low-molecular-weight mebendazole derivatives, differing in their inner structure, and two polymer conjugates differing in their linker structure, were synthesized. The overall synthetic strategy was designed to enable the modification and polymer conjugation of most benzimidazole-based anthelmintics, such as albendazole, fenbendazole or albendazole, besides the mebendazole. Furthermore, the described methodology may be suitable for conjugation of other biologically active compounds with a heterocyclic N-H group in their molecules.

scholarly journals Synthesis and structural features of 5-(4-(tert-butyl) phenyl)-4-((R)amino)-4H-1,2,4-triazole-3-thiols

2018 ◽  
pp. 60-65
Author(s):  
I. I. Aksyonova-Seliuk ◽  
O. I. Panasenko ◽  
E. G. Knysh
Keyword(s):  
Chemical Structure ◽  
Chemical Properties ◽  
Biologically Active ◽  
Physical And Chemical Properties ◽  
Tert Butyl ◽  
New Compounds ◽  
Physical And Chemical ◽  
Derivatives Of ◽  
Active Substances ◽  
And Chemical Properties

Chemistry of heterocyclic compounds is one of the most popular sector in organic chemistry. Scientists allocate among them a class of derivatives of 1,2,4-triazole. This class of compounds attracts attention his broad spectrum of biological activity. There are antiviral, anti-inflammatory, anti-tubercular, antimicrobial, antioxidant, actoprotective, anti-cancer and other activities. The derivatives of 1,2,4-triazole have one more important advantage. It is low toxicity. This properties do this class of derivatives promising for researches their chemical structure and biological activity and purposeful search of biologically active substances. The purpose of the work is synthesis of 5-(4-(tert-butyl)phenyl)-4-((R)amino)-4H-1,2,4-triazoles-3-thiols from appropriate ylidene derivatives of 4-amino-5-(4 (tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol and research of their physical and chemical properties. The objects of research were 10 new compounds, derivatives of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol. These compounds are the crystal substances which are odorless, insoluble in water and soluble in organic solvents. Investigation of the physical and chemical properties of this compounds was carried out according to the methods listed in the State Pharmacopoeia of Ukraine. The melting temperature of synthesized compounds was determined by device OptiMelt Stanford Research Systems MPA100. The structure of the compound was confirmed by 1H-NMR spectroscopy (Mercury 400) and gas chromatography-mass spectrometry (Agilent 1260 Infinity HPLC). 10 new compounds, derivatives of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol, were synthesized in a study. The chemical structure of the new compounds was confirmed by modern instrumental methods of analysis. Results of the done work can be use in the future search of biologically active substances.

scholarly journals Oat β-glucan: physico-chemical characteristics in relation to its blood-glucose and cholesterol-lowering properties

2014 ◽  
Vol 112 (S2) ◽  
pp. S4-S13 ◽  
Author(s):  
Qi Wang ◽  
Peter R. Ellis
Keyword(s):  
Blood Glucose ◽  
Plasma Cholesterol ◽  
Chemical Properties ◽  
Water Soluble ◽  
Biologically Active ◽  
Metabolic Effects ◽  
Cholesterol Lowering ◽  
Solution Rheology ◽  
And Storage

The water-soluble, mixed-linkage β-glucan, a form of soluble dietary fibre, is considered the main biologically active component responsible for the capacity of many oat products to lower postprandial glycaemia and fasting plasma cholesterol in human subjects. The present review discusses the physical and chemical properties of oat β-glucan that are considered important predictors of these beneficial metabolic effects.In vitromodelling and animal and human studies have provided compelling evidence showing that the ability of oat β-glucan to increase the viscosity of digesta in the gastrointestinal tract (GIT) is a primary determinant of its blood-glucose and cholesterol-lowering properties. Therefore, the chemical structure, molecular weight (MW), the rate and extent of dissolution and solution rheology of oat β-glucan are key factors in determining the physiological function of oat-containing foods. The structure and properties of oat β-glucan vary between species and varieties of oats, and are also affected by the growing and storage conditions and processing of oat grain. In addition, the extraction and analysis methods may also contribute to the variations in the structure, MW, hydration and solution rheology of β-glucan obtained from different laboratories. Recent work has demonstrated that β-glucan solubility in foods depends on the source of the material and processing conditions; solubility may also be subject to changes during food preparation and storage (such as freezing). In conclusion, both the amount and MW of β-glucan that are solubilised in the GIT need to be considered when assessing the blood-glucose and cholesterol-lowering properties of oat-containing foods.

scholarly journals Synthesis, physical and chemical properties of 5-(phenoxymethylene)-4-R-1,2,4-triazol-3-thiones derivatives, which contain alkyl- and arylnitrile fragments

2018 ◽  
pp. 52-58
Author(s):  
Yu. M. Kucheryavyi ◽  
A. G. Kaplaushenko
Keyword(s):  
Chemical Properties ◽  
Biologically Active ◽  
Physical And Chemical Properties ◽  
Chemical Methods ◽  
The Core ◽  
Physical And Chemical ◽  
Tumor Drugs ◽  
Derivatives Of ◽  
Active Substances ◽  
And Chemical Properties

Ukraine takes the second place in Europe for the dissemination of cancer. Ukrainian pharmaceutical market practically doesn’t have domestic anti-tumor drugs. That’s why, many scientists of pharmaceutical industry work in this direction.  The searching of biologically active substances among derivatives of 1,2,4-triazole is actually for today. Anastrozole and Letrozole are enough known like anti-tumor drugs which contain in their structures the core of 1,2,4-triazole and nitrile groups. The aim of our work is purposeful synthesis a number of new highly effective compounds 2-((5-(phenoxymethylene)-4-R-4H-1,2,4-triazole-3-yl)thio)acetonitriles and 2-, 3-, 4-(((5-(phenoxymethylene)-4-R-4H-1,2,4-triazole-3-yl)thio)methyl)benzo-nitriles, research of its physical and chemical properties. The 5-(phenoxymethylene)-4-R-1,2,4-triazole-3-thiones, which contain alkyl- and arylnitrile groups has been synthesized and its effective methods obtaining have been set. The structure of synthesized compounds has been confirmed by modern complex of physical and chemical methods of analysis. The synthesized compounds with alkyl- and arylnitrile functional groups will become the basis for further modification of the structure to increase results or expand the range of the biological activity.

Biologically Active, Water-soluble Derivatives of Nystatin – Chemical Studies

Chemotherapy ◽  
1963 ◽  
Vol 6 (6) ◽  
pp. 326-343 ◽  
Author(s):  
G. Rapi ◽  
P. Cocchi ◽  
E. Belgodere
Keyword(s):  
Water Soluble ◽  
Biologically Active ◽  
Chemical Studies ◽  
Derivatives Of

scholarly journals Chemical Modification of an Antitumor Alkaloid, 20(S)-Camptothecin. E-Lactone Ring-Modified Water-Soluble Derivatives of 7-Ethylcamptothecin.

1993 ◽  
Vol 41 (2) ◽  
pp. 310-313 ◽  
Author(s):  
Seigo SAWADA ◽  
Takashi YAEGASHI ◽  
Tomio FURUTA ◽  
Teruo YOKOKURA ◽  
Tadashi MIYASAKA
Keyword(s):  
Chemical Modification ◽  
Lactone Ring ◽  
Water Soluble ◽  
Derivatives Of
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