The studies in a series of 2-(benzoylamino)(1-R-2-oxoindoline-3-ylidene) acetic acids and their derivatives have shown that compounds of the isostructural series exhibit the nootropic, antihypoxic, anabolic activity.Aim. To study the reactivity of esters of 2-(benzoylamino)(1-R-2-oxoindoline-3-ylidene) acetic acids. Materials and methods.The concentration of NaOH in the solution was determined by potentiometric titration on an EV-74 ionomer using the standard aqueous HCl solution. The reaction kinetics was performed in triplicates, the experiments contained 6-8 measurements (the depth of the change was not less than 80 %). The accuracy of the results obtained was assessed by the methods of mathematical statistics of small samples with statistical significance of 0.95.Results and discussion. The reaction rate constants of alkaline hydrolysis of esters of 2-(benzoylamino)(1-R-2-oxoindoline-3-ylidene) acetic acids depend on the structure and the length of the hydrocarbon chain at the heterocyclic nitrogen atom. Introduction of hydrocarbon radicals to the structure of the heterocycle slows down the reaction, while the chain extension accelerates it. The effect of the electronic nature of the substituents on the reactivity of ethyl esters was quantitatively assessed by Hammett equation. The data obtained suggest that the values of the reaction parameter ρ are positive in the temperature range studied; it is additionally confirmed by the В АС 2 mechanism of this reaction.Conclusions. The reaction kinetics of alkaline hydrolysis of biologically active ethyl esters of 2-(benzoylamino) (1-R-2-oxoindoline-3-ylidene) acetic acids has been studied in a wide temperature range; its В АС 2 mechanism has been proven with formation of highly symmetrical intermediate. The effect of the substituents at the heterocyclic nitrogen atom on the numerous kinetic and activation parameters of the reaction has been analyzed; isokineticity and synchronicity of the reaction have been proven using independent tests. Реакційна здатність етилових естерів 2-(бензоїламіно)(1-R-оксоіндолін-3-іліден) оцтових кислотДослідження в ряду 2-(бензоїламіно)(1-R-2-оксоіндолін-3-іліден)оцтових кислот та їх похідних показали, що сполуки цих ізоструктурних рядів проявляють ноотропну, антигіпоксичну, анаболічну активність.Мета роботи -дослідження реакційної здатності естерів 2-(бензоїламіно)(1-R-2-оксоіндолін-3-іліден)оцто-вих кислот.Матеріали та методи. Концентрацію NaOH у розчині визначали потенціометричним титруванням на іономірі EV-74 стандартним водним розчином HCl. Кінетику реакції вивчали у трикратному повторенні, досліди містили 6-8 вимірів (глибина перетворень -не менше 80 %). Оцінку точності одержаних результатів здійснювали мето-дом математичної статистики малих вибірок при достовірній ймовірності 0,95.Результати та їх обговорення. Константи швидкості реакції лужного гідролізу естерів 2-(бензоїламіно) (1-R-2-оксоіндолін-3-іліден)оцтових кислот залежать від структури та довжини вуглеводневого ланцюга при гетеро-циклічному атомі нітрогену. Введення до...
Aim. Today, there are a lot of dietary supplements with lingonberry at the pharmaceutical market of Ukraine; therefore, the analysis and quality control of these products are relevant. In this connection, the aim of the research was to study the qualitative composition and determine the quantitative content of phenolic compounds in dietary supplements with lingonberry.Materials and methods. Such dietary supplements as “Extract of lingonberry” (MEDAGROPROM), “Lingonberry” (Danikafarm), “Lingonberry nano” (LSS SYSTEM) were chosen for the study. The qualitative analysis was performed by thin layer chromatography (TLC), spectrophotometry was used for the quantitative determination.Results and discussion. Hydroquinone derivatives, flavonoids and hydroxycinnamic acids were found in the dietary supplements analyzed. The total content of phenolic compounds was 8.70, 0.26, 0.30 %, flavonoids – 6.37, 0.15, 0.12 %, hydroxycinnamic acids – 0.94, 0.06, 0.13 %, and hydroquinone derivatives – 1.01, 0.04, 0.03 % in such dietary supplements as “Extract of lingonberry” (MEDAGROPROM), “Lingonberry” (Danikafarm), “Lingonberry nano” (LSS SYSTEM), respectively. Conclusions. The qualitative and quantitative analysis of the dietary supplements with lingonberry analyzed has been performed. “Extract of lingonberry” (MEDAGROPROM) dietary supplement meets the requirements of the State of Pharmacopoeia of Ukraine 2.0, whereas “Lingonberry” (Danikafarm) and “Lingonberry nano” (LSS SYSTEM) do not. Based on the results of the study it can be concluded that the problem of compliance of dietary supplements is relevant today and requires the introduction of regulatory documentation for the detection and determination of biologically active substances in dietary supplements.
To analyze the persuasive design of advertising as a now days phenomenon, and also to consider the influence of design meanings-images on the perception processes and behavioral reactions of a person
Using on-line services and the ChemBioOffice2014 software package the values of the partition coefficients of some N-R-amine derivatives have been calculated. To identify the quantitative relationships and select the optimal algorithm of calculations the correlation and regression analysis of the values obtained has been conducted. Statistically significant values of correlation for the partition coefficients calculated have been determined. It has been shown that it is advisable to use the value AlogPs for further application.Lipophilicity is one of the criteria for assessing the similarity of synthetic substances and drugs, and it affects the biological activity of substances [9,13,14]. The partition coefficient of n-octanol-water (logP) characterizes physicochemical properties of substances in solutions and is used to simulate their behaviour in the body [3,14]. Distribution and redistribution of substances between lipophilic (fatty) and aqueous phases are part of biological processes, in particular transmembrane transport through lipid layers [11]. Hydrophobicity plays an important role in determining distribution of a substance in the body after absorption, its metabolic rate and elimination. The hydrophobic effect is essential for binding of drugs with their receptors [13].The ability to predict biological properties of compounds through their lipophilicity allows to optimize the search for new drugs and is often included in equations for calculations of the quantitative structure -activity relationships (QSAR) [16].The value logP is experimentally determined by the classical method of measuring distribution of organic compounds between the non-polar phase and water [14] using chromatographic [18], electrochemical [23] and other methods.However, experimental methods to determine logP are time-consuming and expensive, and the values obtained often differ due to the influence of many factors. Therefore, today a significant number of algorithms for theoretical calculations of values logP implemented using the appropriate software [5, 6, 8, 17,24, 25].The values of the partition coefficients of n-octanolwater experimentally obtained with the values theoretically calculated by different algorithms (AlogPs, IAlogP, ClogP, miLogP, logP KowWIN , xlogP3, etc.) were compared for 193 substances [19] and more than 96 000 compounds (including databases of Nykomed and Pfizer) [15]. In both studies the experimental data better correlate with the methods of AlogPs, xlogP3, logP KowWIN .Attempts to achieve proportionality of results of the theoretical calculation methods of prediction and the experimental determination of lipophilicity of organic compounds are still relevant in modern scientific studies [1, 16, 22].The aim of this work is to determine the mutual correlation of the values of the partition coefficients in the series of some functional derivatives of N-R-amines (1-21) calculated by different algorithms. Materials and MethodsTaking into account the data [15,19] we used the available free on-line methods xlog...
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