scholarly journals Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6579
Author(s):  
Artemiy Nichugovskiy ◽  
Gian Cesare Tron ◽  
Mikhail Maslov

Biogenic polyamines (PAs) are involved in the growth and development of normal cells, and their intracellular concentration is stable. The concentration of PAs in cancer cells is significantly increased to promote and sustain their rapid proliferation. Over the years, synthetic PAs, which differ in their structure, have demonstrated high antitumor activity and are involved in clinical trials. The chemical synthesis of PAs and their conjugates require the correct choice of synthetic pathways—methods for constructing conjugates and the orthogonal protection of amino groups. The most common methods of synthesis of PA conjugates are acylation of regioselectively protected PAs or their alkylation under the conditions of the Fukuyama reaction. One of the most promising methods of PA synthesis is the use of a multicomponent Ugi reaction, which allows various PAs to be obtained in high yields. In this review, we describe and analyze various approaches that are used in the synthesis of polyamines and their conjugates.

2021 ◽  
pp. 30-38

The development of new methods of synthesis using cheaper reagents for the preparation of maleic acid derivatives, the study of chemical properties and the determination of new directions for the practical application of maleic acid derivatives are still relevant. Therefore, the development of this work is an urgent task. The aim of this study was to obtain the synthesis of monomaleinamide compounds under various conditions to obtain arylmaleimide derivatives of maleic acid and to transfer them in a pure state for further reactions. In this study, scientific studies were carried out to find convenient methods for the preparation of monoamide compounds of maleic acid based on equimolar reactions of aromatic monoamines with functional groups -OH, -COOH, -NO2 with maleic anhydride and maleic acid in the meta-state, and the reaction conditions were analyzed. The relative activity of amines in nucleophilic binding reactions is following an order: (-OH <-COOH <-NO2). According this order, the m-nitroaniline was found to be more active in reaction. The proposed methods were used to study the effect of solvents (dioxane, acetone, DMF, ethanol) on the reaction of monoarylamines with maleic anhydride, as well as on the reaction with maleic acid (acetone, glacial acetic acid) and the effect of different temperatures on the reaction yield. discovered. Aproton showed high yields in the reaction of the solvent with acetone. As a result of the reactions of esterification of arylmaleinamides with methanol and ethanol, the corresponding esters were synthesized. The structure of the obtained compounds was confirmed by IR-, 1H NMR-spectroscopy, gas chromatography-mass spectrometry (GC-MS) and other methods. The level of activity of N-(3-hydroxyphenyl)maleinamide against some microorganisms was studied


Author(s):  
A.C. Kagermazova A.C. ◽  
◽  
O.K. Tsagoeva O.K.

When growing winter malting barley, nitrogen fertilizers, along with the correct choice of varieties, are the most important factor in obtaining high yields and high technological qualities of grain. Our studies have shown that the size and dynamics of leaf surface formation are influenced by the dose and combination of mineral fertilizers. It was determined that the average indicators of photosynthetic activity of plants of the studied varieties are characterized for the better when N30P30 is added to the soil against the background of N45P45K45 in the Mikhailo variety.


Author(s):  
М.Sh. Asfandiyarova ◽  
◽  
Т.P. Rybakova ◽  

In 2017–2018, we studied 45 sesame samples from the VIR collection in the experimental fields of the Cis-Caspian Agrarian Federal Scientific Center of the Russian Academy of Sciences (PAFNC RAN). According to temperature indicators, conditions of the years of a research were favorable for the growth and development of sesame. The sum of positive temperatures over the years was equal 3253.8 and 3249.7 °C, respectively. The length of the vegetative period of samples varied from 104 to 133 days. The earliest maturing samples (98–105 days) were KK-80 and 741 from Uzbekistan and K-802 from Tajikistan. As middle-early maturing (106–115 days) 11 samples were characterized, 25 samples were middle maturing (116–125 days), and five samples were late maturing (126–133 days). The most of the samples (33 samples) had seeds of average size (1000 seeds weight of 3.0–3.4 g) at the standard level (3.1 g). By a complex of economically valuable traits we selected 30 samples. The samples KK-883, 291, 171, 265, 468 from Uzbekistan, Azerbaijan, Turkey, Tunisia and Malta demonstrated the highest yield (3.0–4.3 t/ha). Very early maturing samples of sesame with high yields are of great interest and can be used in breeding work.


2019 ◽  
Vol 23 (10) ◽  
pp. 1158-1165
Author(s):  
Vladimir A. D'yakonov ◽  
Gulnara N. Kadikova ◽  
Guzel F. Gazizullina ◽  
Lilya U. Dzhemileva ◽  
Artur R. Tulyabaev ◽  
...  

Triepoxides were synthesized for the first time in high yields (80-85%) by oxidation of substituted bicyclo[4.2.2]deca-2,4,7,9-tetraenes, bicyclo[4.2.2]deca-2,4,7-trienes, and tricyclo[9.4.2.02,10]heptadeca-2,12,14,16-tetraene with an excess of m-chloroperbenzoic acid. The structures of the epoxy derivatives were reliably proved using modern spectral methods and X-ray diffraction analysis. A high antitumor activity in vitro was found for triepoxides against the Jurkat, K562, U937 tumor cell lines and normal fibroblasts.


2017 ◽  
Vol 6 (3) ◽  
Author(s):  
Igor I. Protsenko ◽  
Linda Zh. Nikoshvili ◽  
Alexey V. Bykov ◽  
Valentina G. Matveeva ◽  
Alexandrina Sulman ◽  
...  

AbstractThis work is devoted to the investigation of the possibility of the use of Ru-containing catalysts on the basis of polymeric matrix of hypercrosslinked polystyrene (HPS) in the hydrogenation of levulinic acid (LA) to gamma-valerolactone (GVL). HPS-based Ru-containing catalysts were synthesized at variation of HPS type (MN100 bearing amino groups or MN270 without functional groups) and metal content. Catalyst 5%-Ru/MN100 was shown to compete with commercial 5%-Ru/C and to allow carrying out the hydrogenation of LA in aqueous medium with high yields of GVL (more than 99%).


2021 ◽  
Vol 17 (1) ◽  
pp. 78-86
Author(s):  
A. G. Galayan ◽  
S. N. Medvedko ◽  
A. V. Bondarev ◽  
V. Y. Chundyshko

The article is devoted to the problem of choosing agricultural machinery, as productive potential of plants depends on its effective operation. The correct choice of parameters and modes of agricultural machinery is the fundamental paradigm for solving this problem. Grain yield is made up of the integration of agricultural machinery and its genetic potential. It is the optimization of the parameters that contributes to the formation of a full-fledged desired, stable yield. In the field, productivity is influenced by many difficult-to-control factors (weather conditions, agrotechnical characteristics of the equipment, seed resistance, etc.). To optimize the process of increasing the productivity of grain, the selection of seed material, its disinfection, as well as sowing using innovative technologies are required. The multi-criterion task of choosing the optimal modes of machinery and the preliminary selection and analysis of high-yielding grain is facilitated by the Harrington function. The object of the research is seven varieties of hard winter wheat, differentiated by the method of Kazakova and Lysogorenko. In 2020 high yields were obtained from the varieties of Amazonka (8,32 t/ha), Kristella (8,27 t/ha), Yantarina (8,07 t/ha), Yakhont (7,81 t/ha). Further analysis of seed material by embryo morphotypes (EMT), maximum and minimum mass of an individual grain was carried out using the Harrington function. A comprehensive assessment of the grains of major and minor EMT has shown that the high-yielding varieties of Amazonka and Christella have an optimal weight of 1000 grains, contain the minimum number of grains with minor EMT and the maximum number of seeds with the main EMT. A comprehensive assessment of sowing equipment showed that the use of this technique affects the yield. So when sowing wheat with the SPM-360 seeder, the declared yield is reduced by 10–15%.


2021 ◽  
Vol 285 ◽  
pp. 02032
Author(s):  
Ryslan Gish ◽  
Anastasiya Zvyagina ◽  
Nina Arakelyan

To obtain high yields of potatoes, plant growth and development regulators of various origins are used. Recently, the use of chemicals made from natural raw materials has become more widespread. One of them is the chemicals Relict based on humic and fulvic acids, which have growth-stimulating adaptogenic and protective properties from peat. It is used both for treatment of tubers before planting, and for vegetative plants treatment. Such treatment allowed to reduce the sparseness in potato plantings, and also contributed to an increase in the yield of large and medium fractions of tubers. The marketability of tubers in the control is 81.7%, and in the areas treated with Relict is higher - at a concentration of 0.01 % - 91.6 %, and by 0.05 % - 93.7 %.


HortScience ◽  
1991 ◽  
Vol 26 (8) ◽  
pp. 1051-1053 ◽  
Author(s):  
A. Benzioni ◽  
S. Mendlinger ◽  
M. Ventura ◽  
S. Huyskens

Seed germination, growth, flowering, and yields of Cucumis metuliferus Mey. were examined in several seasons and conditions in the northern Negev, Israel. Germination was optimal between 20 and 35C. Germination was delayed at 12C, totally inhibited at SC, and greatly inhibited above 35C. Salinity increased the time required for full germination. Plants sown in mid-March set fruit in mid-May and gave a higher yield of export-quality fruits than plants sown in mid-April, which set fruit normally but produced a large proportion of small (<200 g) fruits. Plants sown in June did not flower until October. C. metuliferus sown in a greenhouse on three dates in October and November developed very slowly during the cold months and leaves were chlorotic; however, fast growth and development resumed in the spring and high yields were eventually achieved.


1994 ◽  
Vol 300 (1) ◽  
pp. 277-280 ◽  
Author(s):  
M J Marcote ◽  
D Corella ◽  
C González-Bosch ◽  
J Hernández-Yago

Polyamines induce the transport in vitro of the precursor of ornithine transcarbamylase (pOTC) into isolated rat liver mitochondria by facilitating its functional binding to these organelles. Comparative studies of the effect on the in vitro transport of pOTC of polyamine derivatives and related compounds have allowed us to establish that: (i) at least two protonated amino groups per molecule are necessary to induce the pOTC transport; (ii) a distance of three -CH2- groups between the amino groups in diamines is enough to induce this effect, although no differences were observed with diamines having distances of three to eight -CH2- groups. Longer distances resulted in a marked decrease of the effect.


2021 ◽  
pp. 5-10
Author(s):  
А.Д. Смакуев ◽  
О.И. Власова ◽  
Л.В. Трубачева ◽  
Г.Р. Дорожко

Кукуруза занимает второе место среди зерновых культур, обеспечивая более четверти валового сбора зерна в мире. Важнейший аспект формирования высоких урожаев – технология возделывания культуры, одним из главных элементов которой является основная обработка почвы. Исследования по влиянию двух приёмов обработки почвы (дискования и вспашки) при возделывании трёх гибридов зарубежной и российской селекций (Монсанто DKS 3939, AS-201, Машук 171)на фотосинтетическую деятельность и урожайность кукурузы проводили в условиях Карачаево-Черкесской Республики в 2016–2018 гг. В результате проведённых исследований установлена прямая зависимость между площадью листьев и урожайностью. Максимальную урожайность (7–8 т/га) на вариантах, где применялась вспашка, показал гибрид AS-201. Доказано преимущество вспашки в формировании площади листовой поверхности, о чём свидетельствуют полученные данные и их математическая обработка – BFф> F057,8 : 2,12. Это подчёркивает отзывчивость кукурузы на глубокие отвальные обработки почвы, направленные в полной мере на формирование корневой системы, как следствие – потребление элементов питания и влаги, способствующих формированию вегетативной массы растений, закладке генеративных органов и, в конечном итоге, получению более высокой урожайности в сравнении с поверхностными обработками, такими как дискование. Гибриды Монсанто DKS 3939 и AS-201 на фоне вспашки формировали максимальную продуктивность в благоприятном 2018 году. На вариантах с дисковым лущением такой фактор, как условия года, проявил себя незначительно. Согласно данным исследователей, от основной обработки на 12,2% зависит урожайность культур севооборота. Управляя этим фактором, можно увеличить продуктивность кукурузы на 23…25%. Поэтому правильный выбор системы основной обработки почвы – действенный рычаг повышения урожайности, особенно в современных условиях. При возделывании гибридов кукурузы для получения высоких и стабильных урожаев авторами рекомендуется в качестве основного приёма обработки почвы использовать вспашку. Corn ranks second among cereals, providing more than a quarter of the world's gross grain harvest. The most important aspect of the formation of high yields is the technology of cultivating the crop, one of the main elements of which is the main tillage. Studies on the influence of two tillage techniques (disking and plowing) in the cultivation of three hybrids of foreign and Russian breeding (Monsanto DKS 3939, AS-201, Mashuk 171) on photosynthetic activity and corn yields were carried out in the conditions of the Karachay-Cherkess Republic in 2016–2018. As a result of the conducted researches a direct relationship between the area of leaves and yield was established. The maximum yield (7–8 t/ha) in variants where ploughing was used was shown by the hybrid AS-201. The advantage of plowing in the formation of the leaf surface area has been proved, as evidenced by the obtained data and their mathematical processing – BFf > F05 7.8 : 2.12. This emphasizes the responsiveness of corn to moldboard soil cultivation, fully aimed at the formation of the root system, as a result the consumption of food compounds and moisture elements contributing to the formation of vegetative mass of plants, laying generative organs and, ultimately, obtaining higher yields compared to surface tillage such as disking. Hybrids Monsanto DKS 3939 and AS-201 against the background of ploughing formed maximum productivity in a favorable 2018. On variants with disk husking such a factor as the conditions of the year showed itself insignificantly. According the data of researchers, the yield of crop rotation crops depends on the main tillage by 12.2%. By controlling this factor, one can increase the productivity of corn by 23...25%. Therefore, the correct choice of the main tillage system is an effective lever for increasing yields especially in modern conditions. When cultivating corn hybrids to produce high and stable yields, the authors recommend using ploughing as the main method of tillage practice.


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