scholarly journals Synthesis of new 6-hydroxypyrimidine-4(3Н)-onе derivatives

2020 ◽  
Vol 62 (6) ◽  
pp. 40-43
Author(s):  
Elena V. Kuvaeva ◽  
◽  
Denis A. Kolesnik ◽  
Ksenia E. Kirpikova ◽  
Igor P. Yakovlev ◽  
...  

In this paper, 6-hydroxypyrimidine-4 (3Н)-one derivatives are considered as promising syntones for the creation of new biologically active substances. This is useful since the pyrimidine fragment is a structural component of nucleic acid bases (cytosine, thymine, uracil), uric and orotic acids, coenzymes (flavins and xanthins), a number of vitamins (folic acid, thiamine, pyridoxine, riboflavin). It is worth noting that the pharmaceutical market is widely represented with antitumor (methotrexate, imatinib, tegafur); antiviral (stavudine, zalcitabine, lamivudine, zidovudine, acyclovir, idoxuridine); immunostimulatory (isophone) and sedative drugs (phenobarbital, sodium ethaminal) based on compounds including the pyrimidine cycle. The purpose of the present work is to develop a method for producing new 2,3-diphenyl-5-(alkyl/ phenyl)-6-hydroxypyrimidin-4(3Н)-ones, proving their structure and individuality by NMR spectroscopy and mass spectrometry, elemental analysis and thin-layer chromatography. As a method of producing new 6-hydroxypyrimidin-4(3Н)-ones, a method of condensing N-phenyl-benzenecarboxymidamide with 2-substituted propanedioyldichlorides in the medium of an aprotic non-polar solvent – o-xylene is proposed. The desired products are isolated from the reaction mass using solvent distillation and a reprecipitation method. It was found that maximum yields are achieved with constant stirring of a suspension of N-phenylbenzenecarboxymidamide with a solution of 2-substituted propanedioyl dichloride in o-xylene and further heating of the reaction mass at 144 °C for 4 hours. The individuality of the synthesized compounds was confirmed by thin layer chromatography on Sorbfil® plates in the methanol-dichloroethane (1:9) system, and their structure was proved using modern physicochemical analysis methods: proton magnetic resonance spectroscopy, NMR С13 spectroscopy, mass spectroscopy and elemental analysis.

2019 ◽  
Vol 5 (4) ◽  
pp. 270-277 ◽  
Author(s):  
Vijay Kumar ◽  
Simranjeet Singh ◽  
Ragini Bhadouria ◽  
Ravindra Singh ◽  
Om Prakash

Holoptelea integrifolia Roxb. Planch (HI) has been used to treat various ailments including obesity, osteoarthritis, arthritis, inflammation, anemia, diabetes etc. To review the major phytochemicals and medicinal properties of HI, exhaustive bibliographic research was designed by means of various scientific search engines and databases. Only 12 phytochemicals have been reported including biologically active compounds like betulin, betulinic acid, epifriedlin, octacosanol, Friedlin, Holoptelin-A and Holoptelin-B. Analytical methods including the Thin Layer Chromatography (TLC), High-Performance Thin Layer Chromatography (HPTLC), High-Performance Liquid Chromatography (HPLC) and Liquid Chromatography With Mass Spectral (LC-MS) analysis have been used to analyze the HI. From medicinal potency point of view, these phytochemicals have a wide range of pharmacological activities such as antioxidant, antibacterial, anti-inflammatory, and anti-tumor. In the current review, it has been noticed that the mechanism of action of HI with biomolecules has not been fully explored. Pharmacology and toxicological studies are very few. This seems a huge literature gap to be fulfilled through the detailed in-vivo and in-vitro studies.


Food systems ◽  
2021 ◽  
Vol 4 (1) ◽  
pp. 26-30
Author(s):  
N. V. Kupaeva ◽  
E. R. Vasilevskaya ◽  
L. V. Fedulova ◽  
E. A. Kotenkova

Plants are a rich source of effective non-toxic biologically active substances. Various physicochemical methods of analysis are used for evaluation of plant antioxidant activity. Composition of ethanol extracts of red, yellow and white onion husks, dried rosemary, basil, and chaga were studied by high performance thin layer chromatography (HPTLC) method. The antioxidant activity of the obtained fractions on a chromatographic plate was assessed by subsequent DPPH screening. The extracts red and yellow onion husk and rosemary demonstrated the highest antioxidant activity, variability of the qualitative composition and similarity of antioxidant profiles, while extract of white onion husks did not contain any antioxidant classes. Intensive spots with Rf of 0.13-0.97 were observed along the whole chromatogram track corresponding to red onion husks. It was also found that all tested extract, excepting white onion husk and chaga, contained spots with varying degrees of intensity in the Rf range of 0.96-0.98, which corresponded quercetin Rf value.


2020 ◽  
Vol 19 (5-6) ◽  
pp. 148-154
Author(s):  
Vali A. Sahratov ◽  
Tamara L. Malkova ◽  
Ludmila N. Karpova ◽  
Anna A. Pospelova

The State Pharmacopoeia of the XIV edition defines the approach for the assessment of the quality of medicinal plant materials, it deals with the identification of the main groups of biologically active substances by thin layer chromatography. According to this approach, the analysis of some types of medicinal plant materials as a part of some objects of plant origin was carried out. The article presents the quality assessment algorithm as examplified by peppermint leaves (Mentha piperita L.), which are part of a variety of plant object.


2020 ◽  
Vol 21 (5) ◽  
pp. 1670
Author(s):  
Akhikun Nahar ◽  
Anthony L. Baker ◽  
David S. Nichols ◽  
John P. Bowman ◽  
Margaret L. Britz

In addition to cell membrane phospholipids, Actinobacteria in the order Corynebacteriales possess a waxy cell envelope containing mycolic acids (MA). In optimized culture condition, some species can also accumulate high concentrations of intracellular triacylglycerols (TAG), which are a potential source of biodiesel. Bacterial lipid classes and composition alter in response to environmental stresses, including nutrient availability, thus understanding carbon flow into different lipid classes is important when optimizing TAG synthesis. Quantitative and qualitative analysis of lipid classes normally requires combinations of different extraction, derivatization, chromatographic and detection methods. In this study, a single-step thin-layer chromatography-flame ionization detection (TLC-FID) technique was applied to quantify lipid classes in six sub-Antarctic Corynebacteriales strains identified as Rhodococcus and Williamsia species. A hexane:diethyl-ether:acetic acid solvent system separated the total cellular lipids extracted from cells lysed by bead beating, which released more bound and unbound MA than sonication. Typical profiles included a major broad non-polar lipid peak, TAG and phospholipids, although trehalose dimycolates, when present, co-eluted with phospholipids. Ultra-performance liquid chromatography-tandem mass-spectrometry and nuclear magnetic resonance spectroscopy detected MA signatures in the non-polar lipid peak and indicated that these lipids were likely bound, at least in part, to sugars from cell wall arabinogalactan. Waxy esters were not detected. The single-solvent TLC-FID procedure provides a useful platform for the quantitation and preliminary screening of cellular lipid classes when testing the impacts of growth conditions on TAG synthesis.


1987 ◽  
Vol 33 (1) ◽  
pp. 44-47 ◽  
Author(s):  
N M Kin

Abstract Glycoconjugates were isolated, by repeated chromatography on Biogel P-4, from urine of two patients with different phenotypes of fucosidosis, type I (acute) and type II (chronic). Studies of the isolated compounds with thin-layer chromatography, chromatography on Biogel P-4, gas-liquid chromatography, and 1H- and 13C-nuclear magnetic resonance spectroscopy showed differences in the excretion patterns of fucosyl glycoconjugates in the urine of these patients. The amount of the diglycosylasparagine, fuc alpha 1-6glcNAc-Asn, excreted was significantly lower for the type I than for the type II patient. On the other hand, the reducing hexasaccharide gal beta 1-4(fuc alpha 1-3)glcNAc beta 1-2man alpha 1-3/6man beta 1-4glcNAc was present in much greater quantities in urine from the type I patient. The differences in the excretion patterns of these glycoconjugates may be attributed to different substrate specificities for the residual alpha-L-fucosidases in the two forms of the disease. I propose that such differences may be exploited for the early laboratory diagnosis of the type II form of the disease, particularly by thin-layer chromatography.


Author(s):  
J.V. Guna ◽  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit

2- Methoxy – 6 - {4' - [(4'''- Chlorophenyl) (phenyl) methyl amino] phenyl} - 4 - aryl nicotinonitrile (3a-3l) and 2-Amino-6-{4'-[(4'''-Chlorophenyl)(phenyl)methyl amino]phenyl}-4-aryl nicotinonitrile (4a-4l) have been synthesized. The products have been assayed for their antimicrobial activity against Gram +ve, Gram -ve bacteria and fungi. The structure of the products has been elucidated by IR, 1H-NMR, mass spectral data, elemental analysis and thin layer chromatography.


2018 ◽  
Vol 9 (1) ◽  
Author(s):  
Suzana Apostolov ◽  
Đenđi Vaštag ◽  
Borko Matijević ◽  
Gorana Mrđan

Modern approach in the study of biologically active compounds includes the establishment of relationships between molecular structure, physicochemical properties and the behavior which studied compound can manifest in the biological medium. These examinantions are performed in the early stages of the design of future bioactive agent and require the knowledge of molecular descriptors that can point to its biological activity, including lipophilicity which occupies a key position. For the series of diphenylacetamide derivatives, lipophilicity is determined experimentally by thin-layer chromatography on reversed phase (RP TLC18 F254s), in mixtures of water and various organic modifiers and computationally, by using the relevant software packages. In order to estimate the potential acute toxicity of the tested diphenylacetamide derivatives, their effective concentrations, EC50, on the selected test organisms have been determined. Experimentally determined lipophilicity (RM 0 and m) is correlated with a standard measure of lipophilicity (log P), as well as with the selected parameters of toxicity. Thus it has been found that thin-layer chromatography on reversed phase can be used reliably for describing the lipophilicity and for the evaluation of the toxic effects of diphenylacetamide derivatives.


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