79 research outputs found

    MAKNA SIMBOLIK TRADISI BELAMIN PADA MASYARAKAT DI DESA MULIA KERTA KABUPATEN KETAPANG

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    AbstractThis research aimed to know the symbolic meaning of the tradition of belamin on the community in Mulia Kerta Village, Ketapang Regency. The method used qualitative descriptive. The data source used representative of traditional adat leaders. The techniques of data collections were observation, interviews, and documentation. The results obtain were: 1. This tradition adopted during Hindu culture precisely in the 16th century aimed at cleanse themselves and while the belamin process was taught character education and religious education, 2. The implementation of the tradition of belamin on the community of Desa Mulia Kerta is carrying out through several stages including: the stages of preparation, the stages carried out in the lamin / room, step down lamin, preparation for bathing, doing the betitik process, and the final stage (Khataman Al-Qur'an and Betimbang), 3. In this tradition of belamin there are several values contained such as: the value of divinity education, the value of social and community education, and the value of social and community education.Keywords: Symbolic Meaning, Belamin Tradition, Ketapang Communit

    Pengembangan Media Pembelajaran Mobile Learning Berbasis Android Pada Materi Barisan dan Deret Aritmatika Kelas VIII SMPN 07 Putussibau

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    This research aims to produce Android-based mobile learning learning media on sequence and arithmetic series material for class VIII SMPN 07 Putussibau. This research uses the ADDIE development design model, which consists of five main stages, namely analysis, design, development, implementation and evaluation. The subjects in this research were class VIII students at SMP Negeri 07 Putussibau. The instruments used in this research were validation sheets, questionnaires and tests in the form of essay questions. The results of the research showed that the validity of the Android-based mobile learning learning media on arithmetic sequences and series material was categorized as very valid, the practicality of the Android-based mobile learning learning media on the arithmetic sequences and series material was categorized as very practical, and the Android-based mobile learning learning media on the sequence and series material. arithmetic is categorized as effective

    Topic modelling and emotion analysis of the tweets of British and American politicians on the topic of war in Ukraine

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    This paper focuses on the content and emotive features of four politicians' posts that were published on their official Twitter accounts during the three-month period of the russian invasion of Ukraine. We selected two British politicians – Boris Johnson, the Prime Minister of the UK, and Yvette Cooper, the Labour MP and Shadow Home Secretary of the State for the Home Department – as well as two American politicians, President of the USA Joe Biden and Republican senator Marco Rubio.Β In the first phase, weΒ constructed a dataset containing the tweets of the four politicians, which were selected with regard to the topic of war in Ukraine. To be considered approved, the tweets were supposed to contain such words as Ukraine, russia, war, putin, invasion, spotted in one context. Β In the second phase, we identified the most frequent lexical tokens used by the politicians to inform the world community about the war in Ukraine. For this purpose, we used Voyant Tools, a web-based application for text analysis. These tokens were divided into three groups according to the level of their frequency into most frequent, second most frequent and third most frequent lexical tokens. Additionally, we measured the distribution of the most frequent lexical tokens across the three-month time span to explore how their frequency fluctuated over the study period.Β In the third phase, we analysed the context of the identified lexical tokens, thereby outlining the subject of the tweets. To do this, we extracted collocations using the Natural Language Toolkit (NLTK) library.Β During the final phase of the research, we performed topic modelling using the Gibbs Sampling algorithm for the Dirichlet Multinomial Mixture model (GSDMM) and emotion analysis using the NRC Lexicon library

    ЛСксико-сСмантична рСпрСзСнтація поняття depression Ρƒ сучасній Π°Π½Π³Π»Ρ–ΠΉΡΡŒΠΊΡ–ΠΉ ΠΌΠΎΠ²Ρ– (Lexico-semantic representation of the notion depression in modern English)

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    Π£ статті розглянуто лСксичні ΠΎΠ΄ΠΈΠ½ΠΈΡ†Ρ–, які Ρ€Π΅ΠΏΡ€Π΅Π·Π΅Π½Ρ‚ΡƒΡŽΡ‚ΡŒ поняття дСпрСсії Π² Π°Π½Π³Π»ΠΎΠΌΠΎΠ²Π½Ρ–ΠΉ свідомості. Шляхом ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½ΠΎΠ³ΠΎ ΠΊΠΎΠΌΠΏΠΎΠ½Π΅Π½Ρ‚Π½ΠΎΠ³ΠΎ Π°Π½Π°Π»Ρ–Π·Ρƒ Π±ΡƒΠ»ΠΎ Π²ΠΈΠΎΠΊΡ€Π΅ΠΌΠ»Π΅Π½ΠΎ Ρ‚Ρ– сСмантичні ΠΊΠΎΠΌΠΏΠΎΠ½Π΅Π½Ρ‚ΠΈ, які ΡΠ»ΡƒΠ³ΡƒΡŽΡ‚ΡŒ ΠΌΠ°Ρ€ΠΊΠ΅Ρ€Π°ΠΌΠΈ дСпрСсивного стану Π² сучасній Π°Π½Π³Π»Ρ–ΠΉΡΡŒΠΊΡ–ΠΉ ΠΌΠΎΠ²Ρ–. Для досягнСння сСмантичної однорідності Ρ‚Π° виявлСння відстані, Π½Π° якій ΠΏΠ΅Ρ€Π΅Π±ΡƒΠ²Π°ΡŽΡ‚ΡŒ лСксичні ΠΎΠ΄ΠΈΠ½ΠΈΡ†Ρ– Π² Π·Π°Π΄Π°Π½ΠΎΠΌΡƒ сСмантичному просторі, Π±ΡƒΠ»ΠΎ здійснСно Π²Ρ–Π΄ΠΏΠΎΠ²Ρ–Π΄Π½Ρ– ΠΎΠ±Ρ€Π°Ρ…ΡƒΠ½ΠΊΠΈ, Ρ‰ΠΎ ΡƒΠΌΠΎΠΆΠ»ΠΈΠ²ΠΈΠ»ΠΈ формування ядСрного, основного Ρ‚Π° ΠΏΠ΅Ρ€ΠΈΡ„Π΅Ρ€Ρ–ΠΉΠ½ΠΎΠ³ΠΎ складу лСксико-сСмантичної Π³Ρ€ΡƒΠΏΠΈ. (The article deals with the profound analysis of lexical units that represent the notion of depression in the English language. An effective way of studying the lexical structure of the language is establishing lexico-semantic groups – i.e., words belonging to the same part of speech and describing different aspects of one and the same general notion.. It has been clarified that the lexico-semantic group Β«depressionΒ» presents a set of interconnected linguistic units combined in accordance with specific semes. The fact that the lexeme depression is characterised by a number of semantic components enabled us to apply the filtering mode according to which some specific semes assumed the status of nuclear ones. The analysis of derived linguistic units provides the set of additional semantic components reflecting a wide range of emotional states, moods, symptoms and affects. Measuring the distance at which the lexical units are located in the given semantic space made it possible to define the nuclear, basic and peripheral zones of the investigated lexico-semantic group.

    Changes in the electrical transport of ZnO under visible light

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    Complex impedance spectroscopy data in the frequency range 16Hz < f < 3 MHz at room temperature were acquired on pure ZnO single crystal and thin film. The measured impedance of the ZnO samples shows large changes with time after exposure to or covering them from visible light. At fixed times Cole-Cole-diagrams indicate the presence of a single relaxation process. A simple analysis of the impedance data allows us to obtain two main relaxation times. The behavior for both, ZnO crystal and thin film, is similar but the thin film shows shorter relaxation times. The analysis indicates the existence of two different photo-active defects with activation energies between ~0.8 eV and ~1.1 eV.Comment: 11 pages, 9 figures. Solid state communications, in pres

    Π‘ΠΈΠ½Ρ‚Π΅Π· Ρ‚Π° Π±Ρ–ΠΎΠ»ΠΎΠ³Ρ–Ρ‡Π½Π° ΠΎΡ†Ρ–Π½ΠΊΠ° [[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-3-Ρ–Π»]Π°Ρ†Π΅Ρ‚Π°ΠΌΡ–Π΄Ρ–Π² Π· 1,2,4-ΠΎΠΊΡΠ°Π΄Ρ–Π°Π·ΠΎΠ»ΡŒΠ½ΠΈΠΌ Ρ†ΠΈΠΊΠ»ΠΎΠΌ Ρƒ 6, 7 Ρ‚Π° 8 ΠΏΠΎΠ»ΠΎΠΆΠ΅Π½Π½Ρ–

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    Fused heterocyclic 1,2,4-triazoles have provided much attention due to variety of their interesting biological properties.Aim. To develop the method for the synthesis of novel 2-[(1,2,4-oxadiazol-5-yl)-[1,2,4]triazolo[4,3-a]pyridine-3-yl]acetamides and conduct the biological assessment of the compounds synthesized.Results and discussion. A diverse set of acetamides newly synthesized consists of 32 analogs bearing an 1,2,4-oxadiazole cycle in positions 6, 7 and 8. A convenient scheme of the synthesis starts from commercially available 2-chloropyridine-3-, 2-chloropyridine-4-, 2-chloropyridine-5-carboxylic acids with amidoximes to form the corresponding 2-chloro-[3-R1-1,2,4-oxadiazol-5-yl]pyridines, then follows the reaction ofΒ  hydrazinolysis with an excess of hydrazine hydrate. The process continues via the ester formation with the pyridine ring closure, then the amide formations of the end products are obtained by hydrolysis into acetic acid.Experimental part. A series of new 2-[6-(1,2,4-oxadiazol-5-yl)-, 2-[7-(1,2,4-oxadiazol-5-yl)-, 2-[8-(1,2,4-oxadiazol-5-yl)-[1,2,4]triazolo[4,3-a]pyridine-3-yl]acetamides were obtained in good yields, and their structures were proven by the method of 1H NMR spectroscopy. The prognosis and study of their pharmacological activity were also conducted.Conclusions. The synthetic approach of obtaining the representatives of 2-[(1,2,4-oxadiazol-5-yl)-[1,2,4]triazolo[4,3-a]pyridine-3-yl]acetamides previously unknown can be used as an applicable method for the synthesis of diverse functionalized [1,2,4]triazolo[4,3-a]pyridine derivatives.ΠšΠΎΠ½Π΄Π΅Π½ΡΠΈΡ€ΠΎΠ²Π°Π½Π½Ρ‹Π΅ гСтСроцикличСскиС 1,2,4-Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»Ρ‹ ΠΏΡ€ΠΈΠ²Π»Π΅ΠΊΠ°ΡŽΡ‚ большоС Π²Π½ΠΈΠΌΠ°Π½ΠΈΠ΅ Ρ€Π°Π·Π½ΠΎΠΎΠ±Ρ€Π°Π·ΠΈΠ΅ΠΌ интСрСсных биологичСских свойств.ЦСль Ρ€Π°Π±ΠΎΡ‚Ρ‹. Π Π°Π·Ρ€Π°Π±ΠΎΡ‚Π°Ρ‚ΡŒ ΠΌΠ΅Ρ‚ΠΎΠ΄ синтСза Π½ΠΎΠ²Ρ‹Ρ… 2-[(1,2,4-оксадиазол-5-ΠΈΠ»)- [1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-a]ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»]Π°Ρ†Π΅Ρ‚Π°ΠΌΠΈΠ΄ΠΎΠ² ΠΈ провСсти Π±ΠΈΠΎΠ»ΠΎΠ³ΠΈΡ‡Π΅ΡΠΊΡƒΡŽ ΠΎΡ†Π΅Π½ΠΊΡƒ синтСзированных соСдинСний.Π Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚Ρ‹ ΠΈ ΠΈΡ… обсуТдСниС. Π‘ΠΈΠ½Ρ‚Π΅Π·ΠΈΡ€ΠΎΠ²Π°Π½ ряд Π½ΠΎΠ²Ρ‹Ρ… ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹Ρ… Π°Ρ†Π΅Ρ‚Π°ΠΌΠΈΠ΄ΠΎΠ², ΠΊΠΎΡ‚ΠΎΡ€Ρ‹ΠΉ состоит ΠΈΠ· 32 Π°Π½Π°Π»ΠΎΠ³ΠΎΠ², содСрТащих 1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»ΡŒΠ½Ρ‹ΠΉ Ρ†ΠΈΠΊΠ» Π² 6, 7 ΠΈ 8 полоТСниях. Удобная схСма синтСза начинаСтся с коммСрчСски доступных 2-Ρ…Π»ΠΎΡ€ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½-3, 2-Ρ…Π»ΠΎΡ€ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½-4, 2-Ρ…Π»ΠΎΡ€ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½-5-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²Ρ‹Ρ… кислот с амидоксимами с ΠΎΠ±Ρ€Π°Π·ΠΎΠ²Π°Π½ΠΈΠ΅ΠΌ ΡΠΎΠΎΡ‚Π²Π΅Ρ‚ΡΡ‚Π²ΡƒΡŽΡ‰ΠΈΡ… 2-Ρ…Π»ΠΎΡ€-[3-R1-1,2,4-оксадиазол-5-ΠΈΠ»]ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½ΠΎΠ², послС Ρ‡Π΅Π³ΠΎ слСдуСт рСакция Π³ΠΈΠ΄Ρ€Π°Π·ΠΈΠ½ΠΎΠ»ΠΈΠ·Π° с ΠΈΠ·Π±Ρ‹Ρ‚ΠΊΠΎΠΌ Π³ΠΈΠ΄Ρ€Π°Π·ΠΈΠ½ Π³ΠΈΠ΄Ρ€Π°Ρ‚Π°. ΠŸΡ€ΠΎΡ†Π΅ΡΡ продолТаСтся ΠΏΡƒΡ‚Π΅ΠΌ образования эфира с Π·Π°ΠΊΡ€Ρ‹Ρ‚ΠΈΠ΅ΠΌ ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ ΠΊΠΎΠ»ΡŒΡ†Π°, Π·Π°Ρ‚Π΅ΠΌ Ρ‡Π΅Ρ€Π΅Π· Π³ΠΈΠ΄Ρ€ΠΎΠ»ΠΈΠ· ΠΊ уксусной кислотС ΠΌΡ‹ ΠΏΠΎΠ»ΡƒΡ‡Π°Π΅ΠΌ Π°ΠΌΠΈΠ΄Π½Ρ‹Π΅ образования ΠΊΠΎΠ½Π΅Ρ‡Π½Ρ‹Ρ… ΠΏΡ€ΠΎΠ΄ΡƒΠΊΡ‚ΠΎΠ².Π­ΠΊΡΠΏΠ΅Ρ€ΠΈΠΌΠ΅Π½Ρ‚Π°Π»ΡŒΠ½Π°Ρ Ρ‡Π°ΡΡ‚ΡŒ. Ряд Π½ΠΎΠ²Ρ‹Ρ… 2-[6-(1,2,4-оксадиазол-5-ΠΈΠ»)-, 2-[7-(1,2,4-оксадиазол-5-ΠΈΠ»)-, 2-[8-(1,2,4-оксадиазол-5-ΠΈΠ»)-[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°] ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»]Π°Ρ†Π΅Ρ‚Π°ΠΌΠΈΠ΄ΠΎΠ² Π±Ρ‹Π» ΠΏΠΎΠ»ΡƒΡ‡Π΅Π½ с Ρ…ΠΎΡ€ΠΎΡˆΠΈΠΌΠΈ Π²Ρ‹Ρ…ΠΎΠ΄Π°ΠΌΠΈ, Π° ΠΈΡ… структуры ΠΏΠΎΠ΄Ρ‚Π²Π΅Ρ€ΠΆΠ΄Π΅Π½Ρ‹ ΠΌΠ΅Ρ‚ΠΎΠ΄ΠΎΠΌ ЯМР 1H-спСктроскопии. Π’Π°ΠΊΠΆΠ΅ Π±Ρ‹Π» ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½ ΠΏΡ€ΠΎΠ³Π½ΠΎΠ· ΠΈ ΠΈΠ·ΡƒΡ‡Π΅Π½ΠΈΠ΅ ΠΈΡ… фармакологичСской активности.Π’Ρ‹Π²ΠΎΠ΄Ρ‹. БинтСтичСский ΠΏΠΎΠ΄Ρ…ΠΎΠ΄ получСния Ρ€Π°Π½Π΅Π΅ нСизвСстных прСдставитСлСй 2-[(1,2,4-оксадиазол-5-ΠΈΠ»)-[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ4,3-Π°]ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»]Π°Ρ†Π΅Ρ‚Π°ΠΌΠΈΠ΄ΠΎΠ² ΠΌΠΎΠΆΠ΅Ρ‚ Π±Ρ‹Ρ‚ΡŒ ΠΏΡ€ΠΈΠΌΠ΅Π½Π΅Π½ для синтСза Ρ€Π°Π·Π»ΠΈΡ‡Π½Ρ‹Ρ… Ρ„ΡƒΠ½ΠΊΡ†ΠΈΠΎΠ½Π°Π»ΠΈΠ·ΠΈΡ€ΠΎΠ²Π°Π½Π½Ρ‹Ρ… [1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½ΠΎΠ²Ρ‹Ρ… ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹Ρ….ΠšΠΎΠ½Π΄Π΅Π½ΡΠΎΠ²Π°Π½Ρ– Π³Π΅Ρ‚Π΅Ρ€ΠΎΡ†ΠΈΠΊΠ»Ρ–Ρ‡Π½Ρ– 1,2,4-Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΈ ΠΏΡ€ΠΈΠ²Π΅Ρ€Ρ‚Π°ΡŽΡ‚ΡŒ Π²Π΅Π»ΠΈΠΊΡƒ ΡƒΠ²Π°Π³Ρƒ Π΄ΠΎ сСбС Ρ€Ρ–Π·Π½ΠΎΠΌΠ°Π½Ρ–Ρ‚Π½Ρ–ΡΡ‚ΡŽ Ρ†Ρ–ΠΊΠ°Π²ΠΈΡ… Π±Ρ–ΠΎΠ»ΠΎΠ³Ρ–Ρ‡Π½ΠΈΡ… властивостСй.ΠœΠ΅Ρ‚Π° Ρ€ΠΎΠ±ΠΎΡ‚ΠΈ. Π ΠΎΠ·Ρ€ΠΎΠ±ΠΈΡ‚ΠΈ ΠΌΠ΅Ρ‚ΠΎΠ΄ синтСзу Π½ΠΎΠ²ΠΈΡ… 2-[(1,2,4-оксадіазол-5-Ρ–Π»)-[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-3-Ρ–Π»]Π°Ρ†Π΅Ρ‚Π°ΠΌΡ–Π΄Ρ–Π² Ρ‚Π° провСсти Π±Ρ–ΠΎΠ»ΠΎΠ³Ρ–Ρ‡Π½Ρƒ ΠΎΡ†Ρ–Π½ΠΊΡƒ синтСзованих сполук.Π Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚ΠΈ Ρ‚Π° Ρ—Ρ… обговорСння. Π‘ΠΈΠ½Ρ‚Π΅Π·ΠΎΠ²Π°Π½ΠΎ Π½ΠΈΠ·ΠΊΡƒ Π½ΠΎΠ²ΠΈΡ… ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΡ… Π°Ρ†Π΅Ρ‚Π°ΠΌΡ–Π΄Ρ–Π², яка ΡΠΊΠ»Π°Π΄Π°Ρ”Ρ‚ΡŒΡΡ Π· 32 Π°Π½Π°Π»ΠΎΠ³Ρ–Π², Ρ‰ΠΎ ΠΌΡ–ΡΡ‚ΡΡ‚ΡŒ 1,2,4-ΠΎΠΊΡΠ°Π΄Ρ–Π°Π·ΠΎΠ»ΡŒΠ½ΠΈΠΉ Ρ†ΠΈΠΊΠ» Ρƒ 6, 7 Ρ‚Π° 8 полоТСннях. Π—Ρ€ΡƒΡ‡Π½Π° схСма синтСзу ΠΏΠΎΡ‡ΠΈΠ½Π°Ρ”Ρ‚ΡŒΡΡ Π· ΠΊΠΎΠΌΠ΅Ρ€Ρ†Ρ–ΠΉΠ½ΠΎ доступних 2-Ρ…Π»ΠΎΡ€ΠΎΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-3-, 2-Ρ…Π»ΠΎΡ€ΠΎΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-4-, 2-Ρ…Π»ΠΎΡ€ΠΎΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-5-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²ΠΈΡ… кислот Π· амідоксимами Π· утворСнням Π²Ρ–Π΄ΠΏΠΎΠ²Ρ–Π΄Π½ΠΈΡ… 2-Ρ…Π»ΠΎΡ€ΠΎ-[3-R1-1,2,4-оксадіазол-5-Ρ–Π»]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½Ρ–Π², після Ρ‡ΠΎΠ³ΠΎ ΠΏΠ΅Ρ€Π΅Π±Ρ–Π³Π°Ρ” рСакція Π³Ρ–Π΄Ρ€Π°Π·ΠΈΠ½ΠΎΠ»Ρ–Π·Ρƒ Π· надлишком Π³Ρ–Π΄Ρ€Π°Π·ΠΈΠ½ Π³Ρ–Π΄Ρ€Π°Ρ‚Ρƒ. ΠŸΡ€ΠΎΡ†Π΅Ρ ΠΏΡ€ΠΎΠ΄ΠΎΠ²ΠΆΡƒΡ”Ρ‚ΡŒΡΡ ΡˆΠ»ΡΡ…ΠΎΠΌ утворСння Π΅Ρ„Ρ–Ρ€Ρƒ Π· закриттям ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ ΠΊΡ–Π»ΡŒΡ†Ρ, ΠΏΠΎΡ‚Ρ–ΠΌ Ρ‡Π΅Ρ€Π΅Π· Π³Ρ–Π΄Ρ€ΠΎΠ»Ρ–Π· Π΄ΠΎ ΠΎΡ†Ρ‚ΠΎΠ²ΠΎΡ— кислоти ΠΌΠΈ ΠΎΡ‚Ρ€ΠΈΠΌΡƒΡ”ΠΌΠΎ Π°ΠΌΡ–Π΄Π½Ρ– утворСння ΠΊΡ–Π½Ρ†Π΅Π²ΠΈΡ… ΠΏΡ€ΠΎΠ΄ΡƒΠΊΡ‚Ρ–Π².Π•ΠΊΡΠΏΠ΅Ρ€ΠΈΠΌΠ΅Π½Ρ‚Π°Π»ΡŒΠ½Π° частина. Ряд Π½ΠΎΠ²ΠΈΡ… 2-[6-(1,2,4-оксадіазол-5-Ρ–Π»)-, 2-[7-(1,2,4-оксадіазол-5-Ρ–Π»)-, 2-[8-(1,2,4-оксадіазол-5-Ρ–Π»)-[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-3-Ρ–Π»]Π°Ρ†Π΅Ρ‚Π°ΠΌΡ–Π΄Ρ–Π² Π±ΡƒΠ² ΠΎΡ‚Ρ€ΠΈΠΌΠ°Π½ΠΈΠΉ Π· Π΄ΠΎΠ±Ρ€ΠΈΠΌΠΈ Π²ΠΈΡ…ΠΎΠ΄Π°ΠΌΠΈ, Π° Ρ—Ρ… структури ΠΏΡ–Π΄Ρ‚Π²Π΅Ρ€Π΄ΠΆΠ΅Π½Ρ– ΠΌΠ΅Ρ‚ΠΎΠ΄ΠΎΠΌ ЯМР 1H-спСктроскопії. Π’Π°ΠΊΠΎΠΆ Π±ΡƒΠ»ΠΎ Π·Ρ€ΠΎΠ±Π»Π΅Π½ΠΎ ΠΏΡ€ΠΎΠ³Π½ΠΎΠ· Ρ‚Π° вивчСння Ρ—Ρ… Ρ„Π°Ρ€ΠΌΠ°ΠΊΠΎΠ»ΠΎΠ³Ρ–Ρ‡Π½ΠΎΡ— активності.Висновки. Π‘ΠΈΠ½Ρ‚Π΅Ρ‚ΠΈΡ‡Π½ΠΈΠΉ ΠΏΡ–Π΄Ρ…Ρ–Π΄ Π΄ΠΎ отримання Ρ€Π°Π½Ρ–ΡˆΠ΅ Π½Π΅Π²Ρ–Π΄ΠΎΠΌΠΈΡ… прСдставників 2-[(1,2,4-оксадіазол-5-Ρ–Π»)-[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-3-Ρ–Π»]Π°Ρ†Π΅Ρ‚Π°ΠΌΡ–Π΄Ρ–Π² ΠΌΠΎΠΆΠ΅ Π±ΡƒΡ‚ΠΈ застосований для синтСзу Ρ€Ρ–Π·Π½ΠΎΠΌΠ°Π½Ρ–Ρ‚Π½ΠΈΡ… Ρ„ΡƒΠ½ΠΊΡ†Ρ–ΠΎΠ½Π°Π»Ρ–Π·ΠΎΠ²Π°Π½ΠΈΡ… [1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΈΡ… ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΡ…

    EPIDEMIOLOGICAL MANIFESTATIONS OF PREVALENCE OF GLOMERULAR-TUBULOINTERSTITIAL DISEASES OF KIDNEYS AND URETER IN AREAS WITH DIFFERENT LEVELS OF ANTHROPOGENIC LOAD

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    The article reviews the features of the manifestations of the prevalence of glomerular-tubulointerstitial diseases of kidneys and ureter (GTIDKU) in Ufa, Salavat and Sterlitamak with severe anthropogenic load in comparison with the more prosperous Octyabrskiy. Epidemiological manifestations of GTIDKU were evaluated in children, adolescents, adults and the whole population by average long-term indices in dynamics and some periods of observation. Research results revealed significant differences in the prevalence of manifestations of GTIDKU both between the same groups studied on the analyzed areas and between different cohorts on each of them. Among the studied areas the most unfavorable in relation to the intensity of the prevalence of GTIGKU were not only the most favorable in relation to anthropogenic loads Π‘Ρ€Π΅Π΄ΠΈ ΠΈΠ·ΡƒΡ‡Π°Π΅ΠΌΡ‹Ρ… Ρ‚Π΅Ρ€Ρ€ΠΈΡ‚ΠΎΡ€ΠΈΠΉ наимСньшСС Π½Π΅Π±Π»Π°Π³ΠΎΠΏΠΎΠ»ΡƒΡ‡ΠΈΠ΅ ΠΏΠΎ выраТСнности прСвалСнтности Octyabrskiy, but also in the less burdened Salavat while maximum value of general prevalence of GTIGKU in ecologically unfavorable Ufa. Possible connection of observed manifestations with character of qualitative contents of the environment pollutants in Ufa in comparison with Sterlitamak and Salavat and also necessity of increase of the effectiveness of epidemiological diagnostics of GTIGKU in Sterlitamak, Salavat and Octyabrskiy under generally accepted standards are discussed. At that the attention is paid to the expediency of the organization of epidemiological case-control research for the revealing of groups with the highest risk of development of GTIGKU including chronic pyelonephritis. Specification of these statements will allow to optimize measures of the effective management of this pathology on different levels of providing medical aid for such patients

    MYCOBACTERIOSIS IN THE PRACTICE OF PULMONOLOGISTS AND PHTHISIOLOGISTS

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    Goal ofΒ theΒ study: to investigate the frequency of mycobacteriosis in the practice of pulmonologists and phthisiologists.Materials andΒ methods. The analysis included medical files of 156 patients with various non-specific respiratory diseases and tuberculosis who were examined in 2011-2014 and non-tuberculous mycobacteria were found in their sputum.Results ofΒ theΒ study. pulmonary mycobacteriosis was diagnosed in 93 (59.6%) patients out of 156 who corresponded the criteria of American Thoracic Society and etiotropic treatment was prescribed. While detection of non-tuberculous mycobacteria in the other patients was considered as innidiation of respiratory tract by those mycobacteria in case of chronic non-specific pulmonary disease and/or tuberculosis. Mycobacterioses were treated with the relevance to drug susceptibility of the causative agent and there were numerous obstacles due to high frequency of adverse reactions

    IMMUNE-INFLAMMATORY MARKERS of CHRONIC PYELONEPHRITIS

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    The article presents the result of the detection of different-level inflammatory factors of immune defense in patients with chronic pyelonephritis (CP) with detection of definite interconnections between these factors and estimation of their significance in the chronification of the process. The absence of adequate effector reaction on the chronic inflammation with considerable (p < 0,05-0,001) depression of the phagocytosis system, decrease of stimulated reaction of blast-transformed lymphocytes, CD4-helpers, CD16-cells, cytotoxic lymphocytes (CD8), B-lymphocytes (CD22) with oppression of especially secondary immune response against the background of visible (p < 0,05-0,001) decrease of contents of activated lymphocytes (CD25), apoptosis receptors (CD95), antigene of main complex of histocompatibility of 11 class HLADR+, adhesive molecules ICAM-3 and proinflammatory cytokines IL-1β, IL-6, IL-8, ЀНО-α was determined. The character of determined changes in the contents of immune-inflammatory markers that reflect different levels of immune system functioning points at profound disorders of effector reaction with significant oppression of recognition function and destruction by immune system of both endogenous and exogenous antigens and evident inconsistency of cytokines regulatory system in CP patients

    ΠŸΠΎΡˆΡƒΠΊ Π½ΠΎΠ²ΠΈΡ… ΠΏΠΎΡ‚Π΅Π½Ρ†Ρ–ΠΉΠ½ΠΈΡ… Ρ–Π½Π³Ρ–Π±Ρ–Ρ‚ΠΎΡ€Ρ–Π² ΠΏΡ€ΠΎΡ‚Π΅Ρ—Π½ΠΊΡ–Π½Π°Π·ΠΈ Pim-1 сСрСд Π°ΠΌΡ–Π΄Ρ–Π² 1,2,4-Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-3-ΠΌΠ΅Ρ‚Π°Π½Π°ΠΌΡ–Π½Ρƒ Π· 1,2,4-ΠΎΠΊΡΠ°Π΄Ρ–Π°Π·ΠΎΠ»ΡŒΠ½ΠΈΠΌ Ρ†ΠΈΠΊΠ»ΠΎΠΌ Ρƒ 7 Ρ‚Π° 8 полоТСннях

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    The Pim-1 enzyme from the serine/threonine protein kinase family is a likely target for the targeted therapy of tumors of hematopoietic and lymphoid tissues. Triazolopyridine is an universal scaffold upon which international scientific programs have been launched to develop potential anticancer agents.Aim. To create a pharmacophore model to find new potential Pim-1 inhibitors; conduct a virtual screening of a simulated base of new 1,2,4-triazolo[4,3-a]pyridine derivatives; develop a method for the synthesis of 1,2,4-triazolo[4,3-a]pyridine-3-methanamines with the 1,2,4-isoxadiazole cycle.Results and discussion. In this study, a ligand-based pharmacophore model for Pim-1 inhibitors was constructed and validated. A virtual screening of the library with 912 compounds resulted in a hit list of 175 compounds. For the synthesis, 15 compounds were selected with the highest pharmacophore-fit score. 15 compounds were synthesized as potential inhibitors of Pim-1 kinase.Experimental part. The synthetic approach has been developed, and systematic series of new amides of (7-(1,2,4-oxadiazol-5-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)methanamine and (8-(1,2,4-oxadiazol-5-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)methanamine have been synthesized.Conclusions. The compounds obtained are potential inhibitors of Pim-1 kinase. Further studies will focus on the determination of the antitumor activity of the compounds synthesized by in vitro and in vivo methods.Π€Π΅Ρ€ΠΌΠ΅Π½Ρ‚ Pim-1 ΠΈΠ· сСмСйства сСрин/Ρ‚Ρ€Π΅ΠΎΠ½ΠΈΠ½ ΠΏΡ€ΠΎΡ‚Π΅ΠΈΠ½ΠΊΠΈΠ½Π°Π·Ρ‹ являСтся вСроятной мишСнью для Ρ‚Π°Ρ€Π³Π΅Ρ‚Π½ΠΎΠΉ Ρ‚Π΅Ρ€Π°ΠΏΠΈΠΈ ΠΎΠΏΡƒΡ…ΠΎΠ»Π΅ΠΉ ΠΊΡ€ΠΎΠ²Π΅Ρ‚Π²ΠΎΡ€Π½ΠΎΠΉ ΠΈ Π»ΠΈΠΌΡ„ΠΎΠΈΠ΄Π½ΠΎΠΉ Ρ‚ΠΊΠ°Π½Π΅ΠΉ. Π’Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½Ρ‹ – это ΡƒΠ½ΠΈΠ²Π΅Ρ€ΡΠ°Π»ΡŒΠ½Ρ‹ΠΉ скаффолд, Π½Π° Π±Π°Π·Π΅ ΠΊΠΎΡ‚ΠΎΡ€ΠΎΠ³ΠΎ проводятся ΠΌΠ΅ΠΆΠ΄ΡƒΠ½Π°Ρ€ΠΎΠ΄Π½Ρ‹Π΅ Π½Π°ΡƒΡ‡Π½Ρ‹Π΅ ΠΏΡ€ΠΎΠ³Ρ€Π°ΠΌΠΌΡ‹ ΠΏΠΎ Ρ€Π°Π·Ρ€Π°Π±ΠΎΡ‚ΠΊΠ΅ ΠΏΠΎΡ‚Π΅Π½Ρ†ΠΈΠ°Π»ΡŒΠ½Ρ‹Ρ… ΠΏΡ€ΠΎΡ‚ΠΈΠ²ΠΎΡ€Π°ΠΊΠΎΠ²Ρ‹Ρ… срСдств.ЦСль. Π‘ΠΎΠ·Π΄Π°Ρ‚ΡŒ Ρ„Π°Ρ€ΠΌΠ°ΠΊΠΎΡ„ΠΎΡ€Π½ΡƒΡŽ модСль для поиска Π½ΠΎΠ²Ρ‹Ρ… ΠΏΠΎΡ‚Π΅Π½Ρ†ΠΈΠ°Π»ΡŒΠ½Ρ‹Ρ… ΠΈΠ½Π³ΠΈΠ±ΠΈΡ‚ΠΎΡ€ΠΎΠ² Pim-1. ΠŸΡ€ΠΎΠ²Π΅ΡΡ‚ΠΈ Π²ΠΈΡ€Ρ‚ΡƒΠ°Π»ΡŒΠ½Ρ‹ΠΉ скрининг смодСлированной Π±Π°Π·Ρ‹ Π½ΠΎΠ²Ρ‹Ρ… ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹Ρ… 1,2,4-Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½ΠΎΠ² ΠΈ Ρ€Π°Π·Ρ€Π°Π±ΠΎΡ‚Π°Ρ‚ΡŒ ΠΌΠ΅Ρ‚ΠΎΠ΄ синтСза Π°ΠΌΠΈΠ΄ΠΎΠ² 1,2,4-Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½-3-ΠΌΠ΅Ρ‚Π°Π½Π°ΠΌΠΈΠ½Π°, содСрТащих 1,2,4-ΠΈΠ·ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»ΡŒΠ½Ρ‹ΠΉ Ρ†ΠΈΠΊΠ».Π Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚Ρ‹ ΠΈ обсуТдСниС. Π‘ΠΎΠ·Π΄Π°Π½Π° ΠΈ Π²Π°Π»ΠΈΠ΄ΠΈΡ€ΠΎΠ²Π°Π½Π° фармакофорная модСль ΠΈΠ½Π³ΠΈΠ±ΠΈΡ‚ΠΎΡ€ΠΎΠ² Pim-1 Π½Π° основС извСстной ΠΈΠ½Ρ„ΠΎΡ€ΠΌΠ°Ρ†ΠΈΠΈ ΠΎ структурах Π°ΠΊΡ‚ΠΈΠ²Π½Ρ‹Ρ… Π»ΠΈΠ³Π°Π½Π΄ΠΎΠ². ΠŸΡ€ΠΎΠ²Π΅Π΄Π΅Π½ Π²ΠΈΡ€Ρ‚ΡƒΠ°Π»ΡŒΠ½Ρ‹ΠΉ скрининг Π±ΠΈΠ±Π»ΠΈΠΎΡ‚Π΅ΠΊΠΈ ΠΈΠ· 912 соСдинСний, Ρ€Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚ΠΎΠΌ ΠΊΠΎΡ‚ΠΎΡ€ΠΎΠ³ΠΎ стал список Ρ…ΠΈΡ‚ΠΎΠ² ΠΈΠ· 175 соСдинСний. Для синтСза Π±Ρ‹Π»ΠΈ ΠΎΡ‚ΠΎΠ±Ρ€Π°Π½Ρ‹ 15 соСдинСний с Π½Π°ΠΈΠ±ΠΎΠ»Π΅Π΅ высокой Ρ„Π°Ρ€ΠΌΠ°ΠΊΠΎΡ„ΠΎΡ€Π½ΠΎΠΉ ΠΎΡ†Π΅Π½ΠΊΠΎΠΉ. Π‘ΠΈΠ½Ρ‚Π΅Π·ΠΈΡ€ΠΎΠ²Π°Π½Ρ‹ 15 соСдинСний, ΡΠ²Π»ΡΡŽΡ‰ΠΈΡ…ΡΡ ΠΏΠΎΡ‚Π΅Π½Ρ†ΠΈΠ°Π»ΡŒΠ½Ρ‹ΠΌΠΈ ΠΈΠ½Π³ΠΈΠ±ΠΈΡ‚ΠΎΡ€Π°ΠΌΠΈ ΠΊΠΈΠ½Π°Π·Ρ‹ Pim-1.Π­ΠΊΡΠΏΠ΅Ρ€ΠΈΠΌΠ΅Π½Ρ‚Π°Π»ΡŒΠ½Π°Ρ Ρ‡Π°ΡΡ‚ΡŒ. Π Π°Π·Ρ€Π°Π±ΠΎΡ‚Π°Π½Π° схСма, ΠΌΠ΅Ρ‚ΠΎΠ΄ΠΈΠΊΠΈ синтСза ΠΈ синтСзированы систСматичСскиС ряды Π½ΠΎΠ²Ρ‹Ρ… Π°ΠΌΠΈΠ΄ΠΎΠ² (7-(1,2,4-оксадиазол-5-ΠΈΠ»)-[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»)ΠΌΠ΅Ρ‚Π°Π½Π°ΠΌΠΈΠ½Π° ΠΈ (8-(1,2,4-оксадиазол-5-ΠΈΠ»)-[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»)ΠΌΠ΅Ρ‚Π°Π½Π°ΠΌΠΈΠ½Π°.Π’Ρ‹Π²ΠΎΠ΄Ρ‹. ΠŸΠΎΠ»ΡƒΡ‡Π΅Π½Π½Ρ‹Π΅ соСдинСния ΡΠ²Π»ΡΡŽΡ‚ΡΡ ΠΏΠΎΡ‚Π΅Π½Ρ†ΠΈΠ°Π»ΡŒΠ½Ρ‹ΠΌΠΈ ΠΈΠ½Π³ΠΈΠ±ΠΈΡ‚ΠΎΡ€Π°ΠΌΠΈ ΠΊΠΈΠ½Π°Π·Ρ‹ Pim-1. Π”Π°Π»ΡŒΠ½Π΅ΠΉΡˆΠΈΠ΅ исслСдования Π±ΡƒΠ΄ΡƒΡ‚ Π½Π°ΠΏΡ€Π°Π²Π»Π΅Π½Ρ‹ Π½Π° выявлСниС ΠΏΡ€ΠΎΡ‚ΠΈΠ²ΠΎΠΎΠΏΡƒΡ…ΠΎΠ»Π΅Π²ΠΎΠΉ активности синтСзированных соСдинСний ΠΌΠ΅Ρ‚ΠΎΠ΄Π°ΠΌΠΈ in vitro ΠΈ in vivo.Π€Π΅Ρ€ΠΌΠ΅Π½Ρ‚ Pim-1 Π· сімСйства сСрин/Ρ‚Ρ€Π΅ΠΎΠ½Ρ–Π½ ΠΏΡ€ΠΎΡ‚Π΅Ρ—Π½ΠΊΡ–Π½Π°Π· Ρ” ΠΉΠΌΠΎΠ²Ρ–Ρ€Π½ΠΎΡŽ ΠΌΡ–ΡˆΠ΅Π½Π½ΡŽ для Ρ‚Π°Ρ€Π³Π΅Ρ‚Π½ΠΎΡ— Ρ‚Π΅Ρ€Π°ΠΏΡ–Ρ— ΠΏΡƒΡ…Π»ΠΈΠ½ ΠΊΡ€ΠΎΠ²ΠΎΡ‚Π²ΠΎΡ€Π½ΠΎΡ— Ρ‚Π° Π»Ρ–ΠΌΡ„ΠΎΡ—Π΄Π½ΠΎΡ— Ρ‚ΠΊΠ°Π½ΠΈΠ½ΠΈ. Π’Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½ΠΈ – Ρ†Π΅ ΡƒΠ½Ρ–Π²Π΅Ρ€ΡΠ°Π»ΡŒΠ½ΠΈΠΉ скафолд, Π½Π° Π±Π°Π·Ρ– якого Ρ€Π΅Π°Π»Ρ–Π·ΡƒΡŽΡ‚ΡŒΡΡ ΠΌΡ–ΠΆΠ½Π°Ρ€ΠΎΠ΄Π½Ρ– Π½Π°ΡƒΠΊΠΎΠ²Ρ– ΠΏΡ€ΠΎΠ³Ρ€Π°ΠΌΠΈ Π· Ρ€ΠΎΠ·Ρ€ΠΎΠ±ΠΊΠΈ ΠΏΠΎΡ‚Π΅Π½Ρ†Ρ–ΠΉΠ½ΠΈΡ… ΠΏΡ€ΠΎΡ‚ΠΈΡ€Π°ΠΊΠΎΠ²ΠΈΡ… засобів.ΠœΠ΅Ρ‚Π°. Π‘Ρ‚Π²ΠΎΡ€ΠΈΡ‚ΠΈ Ρ„Π°Ρ€ΠΌΠ°ΠΊΠΎΡ„ΠΎΡ€Π½Ρƒ модСль для ΠΏΠΎΡˆΡƒΠΊΡƒ Π½ΠΎΠ²ΠΈΡ… ΠΏΠΎΡ‚Π΅Π½Ρ†Ρ–ΠΉΠ½ΠΈΡ… Ρ–Π½Π³Ρ–Π±Ρ–Ρ‚ΠΎΡ€Ρ–Π² Pim-1. ΠŸΡ€ΠΎΠ²Π΅ΡΡ‚ΠΈ Π²Ρ–Ρ€Ρ‚ΡƒΠ°Π»ΡŒΠ½ΠΈΠΉ скринінг Π·ΠΌΠΎΠ΄Π΅Π»ΡŒΠΎΠ²Π°Π½ΠΎΡ— Π±Π°Π·ΠΈ Π½ΠΎΠ²ΠΈΡ… ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΡ… 1,2,4-Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½Ρƒ Ρ‚Π° Ρ€ΠΎΠ·Ρ€ΠΎΠ±ΠΈΡ‚ΠΈ ΠΌΠ΅Ρ‚ΠΎΠ΄ синтСзу Π°ΠΌΡ–Π΄Ρ–Π² 1,2,4-Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-3-ΠΌΠ΅Ρ‚Π°Π½Π°ΠΌΡ–Π½Ρƒ, Ρ‰ΠΎ ΠΌΡ–ΡΡ‚ΡΡ‚ΡŒ 1,2,4-Ρ–Π·ΠΎΠΊΡΠ°Π΄Ρ–Π°Π·ΠΎΠ»ΡŒΠ½ΠΈΠΉ Ρ†ΠΈΠΊΠ».Π Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚ΠΈ Ρ‚Π° обговорСння. Π‘Ρ‚Π²ΠΎΡ€Π΅Π½ΠΎ Ρ‚Π° Π²Π°Π»Ρ–Π΄ΠΎΠ²Π°Π½ΠΎ Ρ„Π°Ρ€ΠΌΠ°ΠΊΠΎΡ„ΠΎΡ€Π½Ρƒ модСль Ρ–Π½Π³Ρ–Π±Ρ–Ρ‚ΠΎΡ€Ρ–Π² Pim-1 Π½Π° основі Π²Ρ–Π΄ΠΎΠΌΠΎΡ— Ρ–Π½Ρ„ΠΎΡ€ΠΌΠ°Ρ†Ρ–Ρ— ΠΏΡ€ΠΎ структури Π°ΠΊΡ‚ΠΈΠ²Π½ΠΈΡ… Π»Ρ–Π³Π°Π½Π΄Ρ–Π². ΠŸΡ€ΠΎΠ²Π΅Π΄Π΅Π½ΠΎ Π²Ρ–Ρ€Ρ‚ΡƒΠ°Π»ΡŒΠ½ΠΈΠΉ скринінг Π±Ρ–Π±Π»Ρ–ΠΎΡ‚Π΅ΠΊΠΈ Π· 912 сполук, Ρ€Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚ΠΎΠΌ якого став список Ρ…Ρ–Ρ‚Ρ–Π² Ρ–Π· 175 сполук. Для синтСзу Π±ΡƒΠ»ΠΎ Π²Ρ–Π΄Ρ–Π±Ρ€Π°Π½ΠΎ 15 сполук Π· Π½Π°ΠΉΠ²ΠΈΡ‰ΠΎΡŽ Ρ„Π°Ρ€ΠΌΠ°ΠΊΠΎΡ„ΠΎΡ€Π½ΠΎΡŽ ΠΎΡ†Ρ–Π½ΠΊΠΎΡŽ. Π‘ΠΈΠ½Ρ‚Π΅Π·ΠΎΠ²Π°Π½ΠΎ 15 сполук, Ρ‰ΠΎ Ρ” ΠΏΠΎΡ‚Π΅Π½Ρ†Ρ–ΠΉΠ½ΠΈΠΌΠΈ Ρ–Π½Π³Ρ–Π±Ρ–Ρ‚ΠΎΡ€Π°ΠΌΠΈ ΠΊΡ–Π½Π°Π·ΠΈ Pim-1.Π•ΠΊΡΠΏΠ΅Ρ€ΠΈΠΌΠ΅Π½Ρ‚Π°Π»ΡŒΠ½Π° частина. Π ΠΎΠ·Ρ€ΠΎΠ±Π»Π΅Π½ΠΎ схСму, ΠΌΠ΅Ρ‚ΠΎΠ΄ΠΈΠΊΠΈ синтСзу Ρ‚Π° синтСзовано систСматичні ряди Π½ΠΎΠ²ΠΈΡ… Π°ΠΌΡ–Π΄Ρ–Π² (7-(1,2,4-оксадіазол-5-Ρ–Π»)-[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-3-Ρ–Π»)ΠΌΠ΅Ρ‚Π°Π½Π°ΠΌΡ–Π½Ρƒ Ρ‚Π° (8-(1,2,4-оксадіазол-5-Ρ–Π»)-[1,2,4]Ρ‚Ρ€ΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½-3-Ρ–Π»)ΠΌΠ΅Ρ‚Π°Π½Π°ΠΌΡ–Π½Ρƒ.Висновки. ΠžΡ‚Ρ€ΠΈΠΌΠ°Π½Ρ– сполуки Ρ” ΠΏΠΎΡ‚Π΅Π½Ρ†Ρ–ΠΉΠ½ΠΈΠΌΠΈ Ρ–Π½Π³Ρ–Π±Ρ–Ρ‚ΠΎΡ€Π°ΠΌΠΈ ΠΊΡ–Π½Π°Π·ΠΈ Pim-1. ΠŸΠΎΠ΄Π°Π»ΡŒΡˆΡ– дослідТСння Π±ΡƒΠ΄ΡƒΡ‚ΡŒ спрямовані Π½Π° виявлСння ΠΏΡ€ΠΎΡ‚ΠΈΠΏΡƒΡ…Π»ΠΈΠ½Π½ΠΎΡ— активності синтСзованих сполук ΠΌΠ΅Ρ‚ΠΎΠ΄Π°ΠΌΠΈ in vitro Ρ‚Π° in vivo
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