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

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.

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Essential oils biological activity of the Lippia alba (Verbenaceae) shrub

Revista de Biología Tropical ◽

10.15517/rbt.v68i1.39153 ◽

2020 ◽

Vol 68 (1) ◽

Author(s):

Mailen Ortega Cuadros ◽

Emma E Acosta de Guevara ◽

Ailen D Molina Castillo ◽

Clara Gutiérrez Castañeda ◽

Glorismar Castro Amarís ◽

...

Keyword(s):

Biological Activity ◽

Essential Oils ◽

Biological Activities ◽

Biological Properties ◽

Research Groups ◽

Lippia Alba ◽

Sedative Effects ◽

Aromatic Species ◽

Meta Analyses ◽

The Relationship

Introduction: Lippia alba is an aromatic species belonging to the Verbenaceae family. Its essential oils have been used in different industries, because of its biological properties. Objective: Identify the perspectives of the biotechnological applications of Lippia alba essential oils. Methodology: A scoping review was conducted on the biological activity of Lippia alba essential oils registered until October, 2018 in EBSCO, Embase, Scopus, and Lilacs databases. Results: Chemotypes I and III have been reported for different biological activities from the evaluations performed on microorganisms, fish, arthropods, small mammals, and cell lines; fundamentally associated with antibacterial, antifungal, cytotoxic, antioxidant, and sedative effects, among others. Records focused mainly on the health, fishing industry, and agrifood sectors. Conclusion: Studies on the effect of essential oil are promising, but do not reflect a continuity of the research toward prototypes or finished commercial products. Research groups must unify evaluation methodologies and include in all studies the relationship between phytochemical and biological activity for the meta-analyses to be possible. Likewise, they must join efforts through the National System for Agricultural Innovation (SNIA, for the term in Spanish) to generate finished products that impact upon society and facilitate progress in the country’s bio-economy.

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Synthesis and biological activity of Hepta-O-acetyl-1-O- (2-chloro-3-phenyl thio propyl)-β-D-maltose

GEORGIAN SCIENTISTS ◽

10.52340/gs.2021.11.01 ◽

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.

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Estimation of chromatographic lipophilicity of some D-homo androstene derivatives

Acta periodica technologica ◽

10.2298/apt1546249p ◽

2015 ◽

pp. 249-258

Author(s):

Nada Perisic-Janjic ◽

Katarina Penov-Gasi ◽

Evgenija Djurendic ◽

Marina Savic ◽

Strahinja Kovacevic ◽

...

Keyword(s):

High Performance ◽

Predictive Ability ◽

Reversed Phase ◽

Chromatographic Retention ◽

Acetone Water ◽

Validation Parameters ◽

Structure Retention ◽

Leave One Out ◽

Layer Chromatography ◽

Quantitative Structure Retention Relationship

Quantitative structure-retention relationship (QSRR) method was applied to study the chromatographic behaviour of D-homo-androstene derivatives 1-7. Retention constants (RM 0) of the analysed derivatives were determined by reversed-phase high-performance thin-layer chromatography (RP HPTLC) on C18 plates by using four mobile phase mixtures: methanol-water, acetone-water, acetonitrile-water, and dioxane-water. Correlation analysis based on multiple regression method was applied in order to model chromatographic retention by means of nine different lipophilicity descriptors (logP). The developed QSRR models were cross-validated and high-quality validation parameters were obtained by leave-one-out method. It was found that the derived QSRR models have a good predictive ability.

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Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

Chemistry, Technology and Application of Substances ◽

10.23939/ctas2021.02.047 ◽

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.

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Structural Analysis of Fucoidans

Natural Product Communications ◽

10.1177/1934578x0800301011 ◽

2008 ◽

Vol 3 (10) ◽

pp. 1934578X0800301 ◽

Cited By ~ 13

Author(s):

Maria I. Bilan ◽

Anatolii I. Usov

Keyword(s):

Biological Activity ◽

Structural Analysis ◽

Charge Density ◽

Brown Algae ◽

Uronic Acid ◽

Chemical Structure ◽

Biological Activities ◽

Biological Properties ◽

Sulfated Polysaccharides ◽

New Information

Sulfated polysaccharides of brown algae (“fucoidans”) constitute a wide variety of biopolymers from simple sulfated fucans up to complex heteropolysaccharides composed of several neutral monosaccharides, uronic acid and sulfate. The increased interest in this class of polysaccharides is explained by their high and versatile biological activities, and hence, by their possible use in new drug design. Structural analysis of several fucoidans demonstrates that their biological properties are determined not only by charge density, but also by fine chemical structure, although distinct correlations between structure and biological activity cannot be formulated at present. The aim of this review is to describe the methods of structural analysis currently used in fucoidan chemistry, and to discuss some new information on the structures of fucoidans presented in recent publications.

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Fused 1,5-Naphthyridines: Synthetic Tools and Applications

Molecules ◽

10.3390/molecules25153508 ◽

2020 ◽

Vol 25 (15) ◽

pp. 3508

Author(s):

Carme Masdeu ◽

Maria Fuertes ◽

Endika Martin-Encinas ◽

Asier Selas ◽

Gloria Rubiales ◽

...

Keyword(s):

Organic Chemistry ◽

Biological Activity ◽

Metal Complexes ◽

Biological Activities ◽

Nitrogen Heterocycles ◽

Diels Alder ◽

Nitrogen Compounds ◽

Wide Range ◽

Oxygen Heterocycles ◽

Optical Applications

Heterocyclic nitrogen compounds, including fused 1,5-naphthyridines, have versatile applications in the fields of synthetic organic chemistry and play an important role in the field of medicinal chemistry, as many of them have a wide range of biological activities. In this review, a wide range of synthetic protocols for the construction of this scaffold are presented. For example, Friedländer, Skraup, Semmlere-Wolff, and hetero-Diels-Alder, among others, are well known classical synthetic protocols used for the construction of the main 1,5-naphthyridine scaffold. These syntheses are classified according to the nature of the cycle fused to the 1,5-naphthyridine ring: carbocycles, nitrogen heterocycles, oxygen heterocycles, and sulphur heterocycles. In addition, taking into account the aforementioned versatility of these heterocycles, their reactivity is presented as well as their use as a ligand for metal complexes formation. Finally, those fused 1,5-naphthyridines that present biological activity and optical applications, among others, are indicated.

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MECHANOCHEMICAL ACTIVATION OF PHARMACEUTICAL SUBSTANCES AS A FACTOR FOR MODIFICATION OF THEIR PHYSICAL, CHEMICAL AND BIOLOGICAL PROPERTIES

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i3.32413 ◽

2019 ◽

pp. 118-123 ◽

Cited By ~ 4

Author(s):

A.V. SYROESHKIN ◽

E.V. USPENSKAYA ◽

T.V. PLETENEVA ◽

M.A. MOROZOVA ◽

T.V. MAKSIMOVA ◽

...

Keyword(s):

Biological Activity ◽

Chemical Elements ◽

Raw Materials ◽

Biological Activities ◽

Biological Properties ◽

Raw Material ◽

Native Form ◽

Preparation Methods ◽

Pharmaceutical Substances ◽

Before And After

Objective: Study the influence of the mechanical preparation methods (grinding, fluidization) of solid pharmaceutical substances (PS) and herbal raw material on their physicochemical properties and biological activities. Methods: Test substances and solvents-Lactose monohydrate (DFE Pharma, Germany). Sodium chloride, bendazol hydrochloride (all Sigma-Aldrich, USA) and herbal raw material (Callisia fragrans). The dispersity and native structure of pharmaceutical substances were analyzed by several methods: optical microscopy–Altami BIO 2 microscope (Russia); low angle laser light scattering (LALLS) method (Malvern Instruments, UK); Spirotox method–Quasichemical kinetic of cell transition of cellular biosensor Spirostomum ambiguum; Fourier-transform infrared spectroscopy–the analysis in the middle IR region was carried out using an IR Cary 630 Fourier spectrometer (Agilent Technologies, USA). The analysis of dried leaves of C. fragrans before and after mechanical activation was performed using Shimadzu EDX-7000 X-ray fluorescence spectrophotometer without mineralization (Shimadzu, Japan). Results: It was established that the mechanical change, such as dispersion and drying, alters the biological activity of PS and herbal raw materials. The observed increase in the influence of the dispersed substance on the biosensor S. ambiguum is quantitatively estimated from the values of the activation energy (obsEa), which turns to be valued 1,5 (P≤0,05) times more than for the native form substance. In the study of the dependence of the availability of chemical elements K, Ca, Zn on the degree of dispersion of herbal raw materials was established a quantitative 4-fold (P≤0,05) increase in the concentration of elements in mechano-activated raw materials. Conclusion: By the example of the biological model of Spirotox (single-celled biosensor S. ambiguum) and herbal raw materials obtained from C. fragrans, the increase of biological activity of PS at the dispersion of initial preparations was proved.

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Synthesis of Some New 2-Methyl -1,4-benzothiazine-3(1H)- one Derivatives as Potential Vasodilators

E-Journal of Chemistry ◽

10.1155/2004/726204 ◽

2004 ◽

Vol 1 (4) ◽

pp. 206-210 ◽

Cited By ~ 4

Author(s):

M. B. Deshmukh ◽

A. R. Mulik ◽

Savita Dhongade-Desai

Keyword(s):

Blood Flow ◽

Biological Activities ◽

Local Environment ◽

Internal Diameter ◽

Fresh Blood ◽

Software Application ◽

Wide Range ◽

Normal Metabolism ◽

Cardiac Disorders ◽

The Relationship

The increase in the internal diameter of a blood vessel that results from relaxation of smooth muscle within the wall of the vessel is vasodilation. This causes an increase in blood flow and a decrease in systemic vascular resistance. Some substances produced by tissue deprived of fresh blood seem to be responsible for the dilation. Many products of metabolism bring about the action, CO2and acids are among them. Dilation of vessels is necessary to restore local environment of tissues and normal metabolism. It may prove to be potential in the treatment of different cardiac disorders like atherosclerosis, where, the blood vessels are narrowed due to deposition of plaque of substances like cholesterol etc. 1,4-benzothiazines have been reported to possess wide range of pharmacological and biological activities. Here, we report the synthesis and biological activity of some new arylidenehydrazino-(1H)-1,4-benzothiazines. The synthesized compounds were subjected to a prediction of biological activities. A software application (PASS) was used for this purpose. The relationship between structure and different biological activities was studied and it was found that the arylidenehydrazino-(1H)-1,4-benzothiazines are expected to be potential vasodilators.

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Synthesis and Biological Activities of Sulfonated Polysaccharides Having Pentofuransidic Structures

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.342-343.721 ◽

2007 ◽

Vol 342-343 ◽

pp. 721-724

Author(s):

Byung Won Kang ◽

T. Yoshida ◽

Jong Baek Lee ◽

S.J. Jeon ◽

H.D. Choi

Keyword(s):

Biological Activity ◽

Biological Activities ◽

Anticoagulant Activity ◽

Polymer Backbone ◽

Molecular Weights ◽

The Relationship ◽

Anti Hiv

In order to elucidate the relationship between the structure and biological activity such as anti-HIV and blood anticoagulant activity, sulfonated polysaccharides and amino-polysaccharides having pentofuranosidic structures were synthesized. These sulfonated polysaccharides had potent anti-HIV activity in spite of low molecular weights, and which was dependent on the degree of sulfonation. For the blood anticoagulant activity, the conformation of polymer backbone and sulfamide group plays an important role on the interactions with the blood anticoagulant factor.

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Coordination Compounds of Platinum and Palladium with Mixed Ligands (Usnic Acid and 1-(o-Tolyl) Biguanide) � Synthesis, Spectral Characterization and Biological Activity

Revista de Chimie ◽

10.37358/rc.20.4.8073 ◽

2020 ◽

Vol 71 (4) ◽

pp. 336-346

Author(s):

Mirela Calinescu ◽

Ovidiu Oprea ◽

Catalina Stoica ◽

Mihai Nita-Lazar ◽

Madalina Mihalache

Keyword(s):

Staphylococcus Aureus ◽

Pseudomonas Aeruginosa ◽

Biological Activity ◽

Coordination Compounds ◽

Antitumor Agents ◽

Biological Activities ◽

Usnic Acid ◽

Biological Properties ◽

Mixed Ligands

Four coordination compounds of Pd(II), Pt(II) and Pt(IV) with usnic acid (H3AU) and 1-(o-tolyl)biguanide (TB) as ligands have been synthesized in view of their potential as antimicrobial, antifungal and antitumor agents. The metal complexes have been characterized by elemental and thermogravimetrical analyses, infrared and electronic spectra. Based on these studies, the following formulas have been proposed for the complexes: [Pd(TB)(H3AU)]PdCl4 (C1), [Pd(TB)(H2AU)] CH3COO (C2), [Pt(TB)(H2AU)Cl2]Cl (C3) and [Pt(TB)(H2AU)]Cl (C4), where H2AU is deprotonated usnic acid. The in vitro biological activities of the new complexes were tested against Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Candida albicans ATCC 10231 and HeLa tumor cells. All complexes were found to have good biological properties and therefore they can be further explored in therapeutic applications.

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