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INFLUENCE OF THE CARBOHYDRATE COMPONENT OF THE SYNTHETIZED HETEROCYCLIC COMPOUNDS ON THEIR BIOLOGICAL ACTIVITY

Authors: Khaperskaya, L.; Sarymzakova, B.; Ibragimova, A.; Sarymzakova, R.;

INFLUENCE OF THE CARBOHYDRATE COMPONENT OF THE SYNTHETIZED HETEROCYCLIC COMPOUNDS ON THEIR BIOLOGICAL ACTIVITY

Abstract

Список литературы: 1. С.А. Арсаков. Синтез некоторых биологически активных соединений пиперидинового ряда [Текст]: статья /Л.С. Хаперская, С.А.Адылов, Ж.М. Медетбекова // Вестник КНУ им. Ж. Баласагына.- 2004 г.,- № 3.- С.59-62. 2. 2.Р.К. Сарымзакова, Ю.А. Абдурашитова, Ж.А. Джаманбаев. Пути снижения токсичности и повышения избирательности лекарственных препаратов // Вестник Москов.Ун.:М.,2006,-Сер.2,-Т.47,-№ 3,-С. 242-244. 3. Ж.А. Джаманбаев, Ю.А. Абдурашитова, Р.К. Сарымзакова, М.Г. Эралиева. Синтез углеводных производных п-аминобензойной кислоты. 4. М.Д. Машковский. Лекарственные средства. Издание 16. //ООО РИА «Новая волна». -2020. -1236с. 5. А.Т. Солдатенков, Н.М. Колядина, И.В. Щендрик. Основы органической химии лекарственных веществ. - М: Мир, - 2013г.- 153с. 6. Г.А. Саинова. Поиск новых фармакологически активных веществ в ряду производных пиперидина. [Текст]: статья Талисбаев Е.Б., Жарменова М.Б. /// Международный научно-исследовательский журнал -2013 г,- №8. - С.12-19. 7. Geng Q. A facile synthesis of N-aryl substituted piperidones / Zhang H, Cao W, Chen Y. // Chinese Journal of Chemistry.- 2011; -27(10): - Р.995. 8. Ajay Kumar K. Piperidone analogs: syntez and their diverse biological applications / Pavithra G., Renuka N., Vasanth Kumar G // International Research Journal of Pharmaceutical and Applied Sciences (IRJPAS). 2012; 2(6):Р. 145-154. 9. Fernando Aznar Stereoselective Synthesis of meso- and cis- 2,6 - diarylpiperidin - 4 - ones catalyzed by L – proline / Ana – Belen Garcia, Noelia Quinones, Maria – Paz Cabai // Synthesis. 2008. V. 3. P. 479 – 484. 10. Хаперская Л.С., Медетбекова Ж.М., Сарымзакова Р.К. Синтез новых биологически активных соединений N-замещенных гамма пиперидонов // Ж. Успехи Совр. естествознания. - 2016, -9 ,- С.38 – 42 11. D.A. Filimonov, A.A Lagunin, Т.А. Gloriozova et.al. Prediction of the biological activity spectra of organic compounds using the PASS online web resource. //Chem. Heterocycl. -2014.-50(3).- p. 444-457 12. В.В. Поройков, А.Д. Филимонов, А.А. Лагунин, и др. Компьютерная оценка спектра биологической активности химических соединений с целью минимизации рисков их применения в медицине // Проблемы оценки риска здоровью населения от воздействия факторов окружающей среды.-М.,2004.-С.167-169. 13. В.В. Поройков , Д.А. Филимонов, Т.А. Глориозова, А.А. и др.. Компьютерное предсказание биологической активности химических веществ: виртуальная хемогиномика.//Вестник ВОГиС.-2009, -том 13, -№1, С.137 – 143. 14. Д. А.Филимонов, В. В. Поройков. Прогноз спектра биологической активности органических соединений // http://www.imbc.msk.ru/PASS/.

Abstract The searching of new biologically active compounds with the highest efficiency and the least side effects is an important goal, the achievement of which has not only scientific, but also humanitarian and economic significance, because this, in fact, is the optimization of synthesis routes. In the research of the pathways for the synthesis of carbohydrate derivatives of heterocyclic compounds of the piperidine series, the reaction of the synthesis of N-glycosylcarbamides using N-aryl glycosides was studied. By computer prediction of biological activity demonstrated, that the introduction of a carbohydrate fragment into a substance with biological activity leads to an increase in its solubility in water, a decrease in toxicity and a change in the major action of drugs. Also, calculations of the probabilities of occurrence of biological activity upon the introduction of fragments of maltose, sucrose and glucose into 2,6-diphenyl-3-isopropylpiperidin-4-one were carried out. Аннотация Поиск новых биологически активных соединений, имеющих наибольшую эффективность и наименьшее количество побочных эффектов, - важная цель, достижение которой имеет не только научное, но и гуманитарное, и экономическое значения, поскольку это, фактически, оптимизация путей синтеза. В ходе исследования путей синтеза углеводных производных гетероциклических соединений пиперидинового ряда изучена реакция синтеза N – гликозилкарбамидов с использованием N – арилгликозидов. Проведение компьютерного прогноза биологической активности показало, что введение углеводного фрагмента в вещество, обладающее биологической активностью, приводит к увеличению его растворимости в воде, понижению токсичности и изменению действия препаратов. Проведены расчеты вероятностей возникновения биологической активности при введении фрагментов мальтозы, сахарозы и глюкозы в 2,6-дифенил-3-изопропилпиперидин-4-он.

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Keywords

synthesis, 2,6-diphenyl-3-isopropylpiperidin-4-one, carbohydrate derivatives of ketones, biological activity, computer prediction, синтез, 2,6-дифенил-3-изопропилпиперидин-4-он, углеводные производные кетонов, биологическая активность, компьютерный прогноз

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popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
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This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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