Бібліотека Вінницького національного медичного університету ім. М.І.Пирогова

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The synthesis and the antimicrobial activity of N¹-substituted 5-amino-4-arylsulfonyl-3-N-phenylaminopyrazoles [Text] / P. V. Tkachenko [et al.] // Вісн. фармації. - 2017. - № 3. - P3-9

MeSH-главная:
ПИРАЗОЛЫ -- PYRAZOLES (химический синтез)
СТРУКТУРА-АКТИВНОСТЬ, ВЗАИМОСВЯЗЬ -- STRUCTURE-ACTIVITY RELATIONSHIP
АНТИБАКТЕРИАЛЬНЫЕ СРЕДСТВА -- ANTI-BACTERIAL AGENTS (химический синтез)
Аннотация: This article is continuation of the development of methods for the synthesis of small molecules based on the structure of 5-aminopyrazole. The synthesis and the antimicrobial activity for a series of new N1-subsituted 5-amino-4-arylsulfonyl-3-N-phenylaminopyrazoles have been described. Aim. To synthesize derivatives of 5-amino-4-arylsulfonyl-3phenylaminopyrazoles and study their antimicrobial and antifungal properties. Materials and methods. The methods of organic synthesis, instrumental methods of organic compounds analysis and methods of microbiological screening were used. Results and discussion. 5-Amino-4-arylsulfonyl-3-phenylaminopyrazoles were prepared by the reaction of arylsulfonylacetonitriles with isothiocyanates in the presence of NaOH and CH3I with further cyclization with hydrazine hydrate. The reaction of this compounds with N-arylchloroacetamides finished a series of N1-substituted 5-amino-4-arylsulfonyl-3-phenylaminopyrazoles. The antibacterial and antifungal properties of the compounds synthesized were studied. Some of the compounds obtained appeared to be potent inhibitors for several pathogenic bacterial and fungal lines. Conclusions. The synthetic scheme for obtaining of N1-substituted 5-amino-4-arylsulfonyl-3-phenylaminopyrazoles, which can be used for creation of a library of compounds for in vitro antimicrobial screening, has been proposed. Some of the compounds synthesized are of certain interest as potential pharmaceutical agents and can be used to develop new antifungal agents
Доп.точки доступа:
Tkachenko, P. V.
Tkachenko, O. V.
Netosova, K. Yu.
Borisov, O. V.
Zhuravel, I. O.
Kazmirchuk, V. V.

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Molecular parameters and the antimicrobial activity of some N-substituted amino acids [Text] / М. Yu. Golik [et al.] // Вісн. фармації. - 2017. - № 3. - P10-15

MeSH-главная:
АМИНОКИСЛОТЫ -- AMINO ACIDS (фармакология)
БИОДОСТУПНОСТЬ -- BIOLOGICAL AVAILABILITY
СТРУКТУРА-АКТИВНОСТЬ, ВЗАИМОСВЯЗЬ -- STRUCTURE-ACTIVITY RELATIONSHIP
АНТИБАКТЕРИАЛЬНЫЕ СРЕДСТВА -- ANTI-BACTERIAL AGENTS
Аннотация: The concept of “drug likeness” is used when developing drugs for a potential biologically active substance, which must meet some specific criteria, in particular it should be bioavailable. The traditional method of “drug likeness” assessment is verification of compliance with Lipinski’s rule. Aim. To determine the compliance of the “drug likeness” concept for some N-substituted amino acids and identify the quantitative “structure – microbiological activity” relationships. Materials and methods. Using ChemOffice 2016 software the physicochemical parameters determining the bioavailability of some N-substituted amino acids were calculated. Determination of the possible correlations and quantitative ratios of the biological activity data experimentally obtained with the molar refraction (MR) values calculated was conducted using STATISTIKA 8 program. Results and discussion. All compounds studied in their physicochemical properties meet the requirements for new BAS at the stage of testing their biological activity (correspond to Lipinski’s rule). The dependence of the microbiological action of some N-substituted amino acids on MR is maximal for compounds, which MR value is in the range of 2.13-4.53. The growth of all microorganisms was observed for unsubstituted amino acids (MR 2.8). The maximum activity of all compounds studied was observed against gram-positive (B. subtilis and S. aureus), and the less activity was against gram-negative microorganisms (E. coli, P. vulgaris, P. aeruginosa) and fungi (C. albicans). It may be associated with the structural peculiarities of the cellular wall. The MR values calculated correlate satisfactorily with the experimental data of the antimicrobial activity of compounds. Conclusions. Statistically significant values of MR correlation with the values of the antimicrobial activity of some N-substituted amino acids against the microorganisms studied have been determined. It quantitatively confirms the presence of the “structure – activity” relationship in this series of compounds
Доп.точки доступа:
Golik, М. Yu.
Kryskiv, О. S.
Komissarenko, A. M.
Kolisnyk, O. V.

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Navruzova, G. F.
The study of biologically active substances of the extract obtained from peach leaves of the tajik variety [Text] / G. F. Navruzova, V. S. Kyslychenko, L. V. Lenchyk // Вісн. фармації. - 2017. - № 3. - P16-20

MeSH-главная:
(химия)
РАСТЕНИЙ ЛИСТЬЯ -- PLANT LEAVES (химия)
РАСТЕНИЙ ЭКСТРАКТЫ -- PLANT EXTRACTS (анализ, стандарты, фармакология)
Аннотация: To study the qualitative composition and the content of biologically active substances (BAS) in the extract obtained from peach leaves grown in Tajikistan, its numerical parameters and choose the parameters for standardization of the extract. Materials and methods. The object of the study was a soft extract obtained from peach leaves of the “Salvey” variety. For standardization the numerical parameters were determined in 5 batches of the extract. A dry residue, the content of heavy metals and microbiological purity were studied in the extract by the methods of the State Pharmacopoeia of Ukraine (SPhU). The qualitative reaction and thin-layer chromatography (TLC) were proposed for identification of the extract. The content of the amount of phenolic compounds, flavonoids and hydroxycinnamic acids was determined using spectrophotometry calculated with reference to gallic acid, rutin and chlorogenic acid, respectively. The content of polysaccharides was determined gravimetrically, and the content of organic acids by titrimetry according to the SPhU monograph “Rosehips”. Results and discussion. A dry residue of the extract was 78.27 ± 0.12 %. The content of heavy metals did not exceed 0.001 %. According to the results of microbiological purity determination the extract met the SPhU requirements. According to the results of the reaction with the solution of Ferrum (III) chloride the presence of phenolic substances was confirmed. During the TLC analysis several spots were observed, one of which appeared at the level of the standard sample of chlorogenic acid. The quantitative content (%) of the following substances was determined in the extract: polysaccharides – 14.74 ± 0.09, organic acids – 3.71 ± 0.09, phenolic compounds – 12.85 ± 0.39, flavonoids – 4.71 ± 0.09, hydroxycinnamic acids – 8.41 ± 0.07. Conclusions. The analysis of BAS of a soft extract from peach leaves has been carried out. The parameters of its standardization have been selected
Доп.точки доступа:
Kyslychenko, V. S.
Lenchyk, L. V.

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Carboxylic acids of phenolic complexes from Veronica teucrium L. [Text] / А. Р. Osmachko [et al.] // Вісн. фармації. - 2017. - № 3. - P21-27

MeSH-главная:
КАРБОНОВЫЕ КИСЛОТЫ -- CARBOXYLIC ACIDS (анализ, выделение и очистка)
ВЕРОНИКА -- VERONICA (химия)
ЖИРНЫЕ КИСЛОТЫ -- FATTY ACIDS (анализ, выделение и очистка)
Аннотация: To compare and study low molecular aliphatic, fatty and aromatic acids of phenolic complexes (PhC) obtained from V. teucrium L. flowers, leaves and rhizomes using chromatography-mass spectrometry. Materials and methods. Phenolic complexes from flowers, leaves and rhizomes were obtained by the exhaustive circulating extraction method in a Soxhlet apparatus. The analysis of methyl esters of acids was performed on a 5973N/6890N MSD/DS Agilent Technologies (USA) chromatograph using the chromatography-mass spectrometry method. The sample injection in a HP-INNOWAX (0.25 mm × 30 m) chromatographic capillary column was performed by a splitless mode. Identification of methyl esters of acids was performed based on the calculation of the equivalent length of the aliphatic chain (ECL) using data from the mass spectra libraries NIST 05 and Willey 2007 in combination with programs for identifying AMDIS and NIST; the retention time of esters was also compared with the retention time of standard compounds (Sigma). The internal standard method was used for quantitative calculations. Results and discussion. As the result of our study low molecular aliphatic, fatty and aromatic acids have been identified in phenolic complexes of V. teucrium L. flowers, leaves and rhizomes for the first time, their quantitative content is as follows: 2.34 % – in the complex from flowers, 2.78 % – in the complex from leaves, and 2.10 % – in the complex from rhizomes. In the phenolic complex from flowers low molecular aliphatic acids (malonic, levulinic, succinic, 3-hydroxy-2-methylglutaric); fatty acids (palmitic and linolenic); aromatic acids (vanillic, р-coumaric and phydroxybenzoic) prevail. The dominant compounds in the phenolic complex from leaves are low molecular aliphatic acids (malonic, levulinic, succinic, 3-hydroxy-2-methylglutaric, malic); fatty acids (palmitic, oleic, linoleic, linolenic); and aromatic acid (ferulic). In the phenolic complex from rhizomes low molecular aliphatic acids (levulinic, succinic, malic); fatty acids (palmitic, stearic, oleic, linoleic, linolenic); aromatic acids (veratric, vanillic, syringic, ferulic) dominate. Conclusions. As the result of our study for the first time the following components have been identified in phenolic complexes: 40 low molecular aliphatic, fatty and aromatic acids – from flowers, 39 – from leaves, 38 – from rhizomes. The content of carboxylic acids in phenolic complexes is 2.34 % – from flowers, 2.78 % – from leaves, 2.10 % – from rhizomes. It has been found that the herbal drug of V. teucrium L. is a source of valuable biologically active acids with different pharmacological effect
Доп.точки доступа:
Osmachko, А. Р.
Kovaleva, А. М.
Ilyina, T. V.
Koshovyi, О. М.

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Litvinova, O. M.
Development of the laboratory technology of the combined pessaries with acyclovir and essential oils [Text] / O. M. Litvinova, Yu. V. Levachkova, V. M. Chushenko // Вісн. фармації. - 2017. - № 3. - P28-33

MeSH-главная:
ПЕССАРИИ -- PESSARIES
ТЕХНОЛОГИЯ ФАРМАЦЕВТИЧЕСКАЯ -- TECHNOLOGY, PHARMACEUTICAL
АЦИКЛОВИР -- ACYCLOVIR
ЭФИРНЫЕ МАСЛА -- OILS, VOLATILE
ПРОТИВОВИРУСНЫЕ СРЕДСТВА -- ANTIVIRAL AGENTS (фармакология)
ГЕРПЕС ГЕНИТАЛЬНЫЙ -- HERPES GENITALIS (лекарственная терапия)
Аннотация: The range of pessaries at the Ukrainian pharmaceutical market is represented by medicines containing substances of the synthetic origin for the treatment of genital herpes (GH). However, combined drugs with a wide range of pharmacological action and minimal side effects for treating GH are practically absent, except for rectal suppositories “Panavir” containing the purified extract from Solanum tuberosum stem. For this reason the question of expansion of the range of pessaries based on substances of the plant or synthetic origin is topical and important. Aim. To develop the laboratory technology of the combined pessaries with acyclovir and essential oils of tea tree and thyme. Materials and methods. The technological process for preparing pessaries was carried out in accordance to the generally accepted rules for preparing suppositories taking into account the nature and physicochemical properties of active pharmaceutical ingredients (API) and excipients. According to the methods of the State Pharmacopoeia of Ukraine (SPhU) the following parameters were determined on the samples of pessaries: description, uniformity, pH, melting point, time of complete deformation, disintegration time, and resistance. Quantitative determination of acyclovir was conducted by the method of absorption spectrophotometry in the UV spectrum at a wavelength of (265 ± 2) nm. The thermogravimetric studies were performed on a Q-1000 derivatograph of F. Paulik, I. Paulik, L. Efdei system. Results and discussion. Based on the biopharmaceutical and pharmacotechnological studies conducted the laboratory technology of the combined pessaries with acyclovir and essential oils of tea tree and thyme has been developed. The complex of experimental studies on selection of the amount of an emulsifier, fineness and the the choice of solvent for acyclovir, the choice of the rational technology for pessaries has been conducted. The technology proposed allows obtaining pessaries in accordance with the requirements of the SPhU. Conclusions. For the first time the laboratory technology of pessaries with acyclovir and essential oils of tea tree and thyme has been developed. The results obtained have shown the prospects for further study of the combined pessaries with acyclovir and essential oils of tea tree and thyme in order to introduce this dosage form into production
Доп.точки доступа:
Levachkova, Yu. V.
Chushenko, V. M.

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Petrovska, L. S.
Peculiarities of thickening of the modern foam base in the acid medium [Text] / L. S. Petrovska, Yu. О. Bezpala, I. I. Baranova // Вісн. фармації. - 2017. - № 3. - P34-38

MeSH-главная:
ТЕХНОЛОГИЯ ФАРМАЦЕВТИЧЕСКАЯ -- TECHNOLOGY, PHARMACEUTICAL (методы)
ДЕТЕРГЕНТЫ -- DETERGENTS
ВЯЗКОСТЬ -- VISCOSITY
Кл.слова (ненормированные):
Пены
Аннотация: A balanced modern foam system involves the use of various condensation mechanisms that provide a stable structure and satisfactory consumer properties. Aim. To substantiate the rational concentrations of viscosity modifiers when developing foam agents at pH of 3.5-4.5. Materials and methods. The foam base developed contains Disodium Laureth-3-Sulfosuccinate, Cocamidopropyl Betain, Coco Glucoside/Glyceryl Oleate, PEG-7 Glyceryl Cocoate, PEG-4 Rapeseedamide, PEG-150 Polyglyceryl-2 Stearate and Laureth-3, purified water. As a pH regulator lactic acid was used; as a preservative the complex containing Triethylene Glycol/Benzyl Alcohol/Propilene Glycol/Methylclorisothiazolinone and Methylisothiazolinone (Nipaguard CMB, “Clariant”, “Clariant Produkte (Deutschland) GmbH”, Germany). Nipagard CMB provides the activity against gram positive and gram negative bacteria, yeasts and molds, is compatible with anionic, cationic and nonionic surfactants, remains fully stable up to pH 8. The physical and chemical methods, including structural and mechanical methods, were used. For greater reliability of the experiments and the practical value of the work the samples of the substances studied were provided by the pharmaceutical research center “Alliance of Beauty” (Kyiv, Ukraine). Results and discussion. The important task when developing foam systems at acidic pH value is the choice of the complex of viscosity modifiers that would provide stability, easy dosing and the ease of use. The study confirmed the need for introduction of an associative gel former (hydroxypropylmethylcellulose) and electrolyte (sodium chloride). Conclusions. According to the results of the studies the necessity of introducing a complex of viscosity modifiers has been proven: one of them provides the electrolyte thickening, and another one the associative thickening of the foam base
Доп.точки доступа:
Bezpala, Yu. O.
Baranova, I. I.

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Nazarkina, V. M.
Analysis of modern approaches to formation of cost price for veterinary preparations [Text] / V. M. Nazarkina, Zh. M. Polova // Вісн. фармації. - 2017. - № 3. - P39-44

MeSH-главная:
ВЕТЕРИНАРНЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА -- VETERINARY DRUGS (экономика)
ЭКОНОМИКА ФАРМАЦЕВТИЧЕСКАЯ -- ECONOMICS, PHARMACEUTICAL
Аннотация: To analyze the modern approaches to cost accounting and calculation of the cost price of veterinary preparations (VP) in order to increase their economic availability. Materials and methods. The regulatory and legal framework and methodological approaches to formation of the cost of production were analyzed. The production and full costs of VP were calculated in order to substantiate the economic feasibility of their manufacturing. The structure of the cost price of VP was analyzed. Results and discussion. The analysis of the modern approaches to pricing on medicines and VP has been carried out. It has been determined that chemical and pharmaceutical enterprises producing medicines and VP use different approaches when accounting the costs and calculating the cost price; as a result, it has a significant impact on the level of prices and the structure of the cost price. The project cost of three new antimastitis VP in the form of cream, solution and spray has been calculated using two different methods. The calculations performed confirm the economic feasibility of introduction of VP into production. Conclusions. Antimastitis products proposed for introduction into production are price competitive. The efficient cost management of VP will allow gaining competitive advantages at the market and providing their economic availability
Доп.точки доступа:
Polova, Zh. M.

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Zarichkova, M. V.
The study of the directions for creation of employee benefits for pharmacy professionals and calculation of the possible cost of the individual components (options) [Text] / M. V. Zarichkova // Вісн. фармації. - 2017. - № 3. - P45-60

MeSH-главная:
ФАРМАЦИЯ -- PHARMACY (кадры)
ФАРМАЦЕВТЫ -- PHARMACISTS
СОЦИАЛЬНОЕ ОБЕСПЕЧЕНИЕ -- SOCIAL SECURITY (экономика)
Аннотация: To study the directions for creation of employee benefits for pharmacy professionals and calculation of the possible cost of the individual components (options) in a pharmacy institution. Materials and methods. The methodological basis of this study is general scientific and applied research methods, including methods of pairwise interactions, methods of multivariate analysis (Data Mining algorithms, Sequence, Association Rules, and Link Analysis), Friedman ANOVA for dependent samples. The abovementioned analyses were conducted using a StatSoft Statistica software package. Results and discussion. Using the methods of multidimensional statistical analysis and Data Mining the interaction between satisfaction with employee benefits in a pharmacy institution by pharmacy professionals (PhP) and the need to provide or review the current employee benefits and general satisfaction with it have been studied. The analysis of association rules has made it possible to identify stable blocks of interactions between individual components (options), which are peculiar to different degree of PhP satisfaction with employee benefits, and determine factors associated to the greatest extent with the poor, medium, high and total PhP satisfaction with employee benefits. Conclusions. The weight loads of individual components (options) of employee benefits have been calculated in order to form the balanced composition and cost. Based on the proposed scheme of the optimal filling of employee benefits the cost calculation has been made for their components (options), which provide the desired total cost of employee benefits estimated taking into account the data from the survey of PhP questionnaires in the pharmacy institutions of different forms of ownership. Four types of expenses have been offered depending on the position held by PhP
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The experimental study of the antihypoxic and antioxidant activity of 5,7-dihydro-1H-pyrrolo-[2,3-d]pyrimidine derivatives [Text] / V. A. Volkovoy [et al.] // Вісн. фармації. - 2017. - № 3. - P61-65

MeSH-главная:
ПИРИМИДИНЫ -- PYRIMIDINES (химический синтез)
АНТИОКСИДАНТЫ -- ANTIOXIDANTS (химический синтез)
(лекарственная терапия)
СТРУКТУРА-АКТИВНОСТЬ, ВЗАИМОСВЯЗЬ -- STRUCTURE-ACTIVITY RELATIONSHIP
Аннотация: To study the antihypoxic and antioxidant activity of 5,7-dihydro-1H-pyrrolo-[2,3-d]pyrimidine derivatives on the models of the experimental pathology. Materials and methods. The study of the antihypoxic activity of 5,7-dihydro-1H-pyrrolo-[2,3-d]pyrimidine derivatives was conducted on the model of acute hemic hypoxia, the antioxidant action was studied on the model of toxic tetrachlorometane hepatitis. Results and discussion. It was found that the activity of compounds KMS-161, KMS-164, KMS-166, KMS-168, KMS-174, KMS-176, KMS-191 was lower compared to mexidol, and the antihypoxic activity of compounds KMS-162, KMS-163, KMS-172, KMS-178, KMS-179, KMS-211, KMS-214, KMS-217 was close and slightly higher than the activity of mexidol in its median effective dose of 100 mg/kg. The marked antihypoxic activity was found in all groups studied. In the “structure – activity” analysis it was found that the antihypoxic activity among derivatives of 5,7-dihydro-1H-pyrrolo-[2,3-d]pyrimidine was caused by their nature, the structure of the radical and the position of the substituent. The presence of the pyrrole ring in the molecule of 5,7-dihydro-1Н-pyrrolo-[2,3-d]pyrimidine led to the increased antihypoxic activity. A comparative analysis of the effectiveness of the objects studied showed that substances with the code of KMS-162, KMS-176, KMS-191, KMS-211, KMS-214, KMS-217 affected most positively on the state of AOS and LPO in conditions of acute hepatitis. Conclusions. In a series of 5,7-dihydro-1Н-pyrrolo-[2,3-d]pyrimidine derivatives the most active was compound KMS-211, which showed the high antihypoxic activity (131 %) in relation to the control group and exceeded the reference drug mexidol by 45 %. Synthetic derivatives of 5,7-dihydro-1H-pyrrolo-[2,3-d]pyrimidine exhibited the antioxidant activity (compound KMS-211 was the most active). The compounds studied may be the basis for the purposeful synthesis of antihypoxants and antioxidants
Доп.точки доступа:
Volkovoy, V. A.
Sevrukov, O. V.
Kolisnyk, S. V.
Derkach, N. V.
Kryzhna, S. I.
Ostapets, M. O.

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