79 research outputs found
MAKNA SIMBOLIK TRADISI BELAMIN PADA MASYARAKAT DI DESA MULIA KERTA KABUPATEN KETAPANG
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
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
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 β 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 β 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
ΠΠ΅ΠΊΡΠΈΠΊΠΎ-ΡΠ΅ΠΌΠ°Π½ΡΠΈΡΠ½Π° ΡΠ΅ΠΏΡΠ΅Π·Π΅Π½ΡΠ°ΡΡΡ ΠΏΠΎΠ½ΡΡΡΡ depression Ρ ΡΡΡΠ°ΡΠ½ΡΠΉ Π°Π½Π³Π»ΡΠΉΡΡΠΊΡΠΉ ΠΌΠΎΠ²Ρ (Lexico-semantic representation of the notion depression in modern English)
Π£ ΡΡΠ°ΡΡΡ ΡΠΎΠ·Π³Π»ΡΠ½ΡΡΠΎ Π»Π΅ΠΊΡΠΈΡΠ½Ρ ΠΎΠ΄ΠΈΠ½ΠΈΡΡ, ΡΠΊΡ ΡΠ΅ΠΏΡΠ΅Π·Π΅Π½ΡΡΡΡΡ ΠΏΠΎΠ½ΡΡΡΡ Π΄Π΅ΠΏΡΠ΅ΡΡΡ Π² Π°Π½Π³Π»ΠΎΠΌΠΎΠ²Π½ΡΠΉ ΡΠ²ΡΠ΄ΠΎΠΌΠΎΡΡΡ. Π¨Π»ΡΡ
ΠΎΠΌ ΠΏΡΠΎΠ²Π΅Π΄Π΅Π½ΠΎΠ³ΠΎ ΠΊΠΎΠΌΠΏΠΎΠ½Π΅Π½ΡΠ½ΠΎΠ³ΠΎ Π°Π½Π°Π»ΡΠ·Ρ Π±ΡΠ»ΠΎ Π²ΠΈΠΎΠΊΡΠ΅ΠΌΠ»Π΅Π½ΠΎ ΡΡ ΡΠ΅ΠΌΠ°Π½ΡΠΈΡΠ½Ρ ΠΊΠΎΠΌΠΏΠΎΠ½Π΅Π½ΡΠΈ, ΡΠΊΡ ΡΠ»ΡΠ³ΡΡΡΡ ΠΌΠ°ΡΠΊΠ΅ΡΠ°ΠΌΠΈ Π΄Π΅ΠΏΡΠ΅ΡΠΈΠ²Π½ΠΎΠ³ΠΎ ΡΡΠ°Π½Ρ Π² ΡΡΡΠ°ΡΠ½ΡΠΉ Π°Π½Π³Π»ΡΠΉΡΡΠΊΡΠΉ ΠΌΠΎΠ²Ρ. ΠΠ»Ρ Π΄ΠΎΡΡΠ³Π½Π΅Π½Π½Ρ ΡΠ΅ΠΌΠ°Π½ΡΠΈΡΠ½ΠΎΡ ΠΎΠ΄Π½ΠΎΡΡΠ΄Π½ΠΎΡΡΡ ΡΠ° Π²ΠΈΡΠ²Π»Π΅Π½Π½Ρ Π²ΡΠ΄ΡΡΠ°Π½Ρ, Π½Π° ΡΠΊΡΠΉ ΠΏΠ΅ΡΠ΅Π±ΡΠ²Π°ΡΡΡ Π»Π΅ΠΊΡΠΈΡΠ½Ρ ΠΎΠ΄ΠΈΠ½ΠΈΡΡ Π² Π·Π°Π΄Π°Π½ΠΎΠΌΡ ΡΠ΅ΠΌΠ°Π½ΡΠΈΡΠ½ΠΎΠΌΡ ΠΏΡΠΎΡΡΠΎΡΡ, Π±ΡΠ»ΠΎ Π·Π΄ΡΠΉΡΠ½Π΅Π½ΠΎ Π²ΡΠ΄ΠΏΠΎΠ²ΡΠ΄Π½Ρ ΠΎΠ±ΡΠ°Ρ
ΡΠ½ΠΊΠΈ, ΡΠΎ ΡΠΌΠΎΠΆΠ»ΠΈΠ²ΠΈΠ»ΠΈ ΡΠΎΡΠΌΡΠ²Π°Π½Π½Ρ ΡΠ΄Π΅ΡΠ½ΠΎΠ³ΠΎ, ΠΎΡΠ½ΠΎΠ²Π½ΠΎΠ³ΠΎ ΡΠ° ΠΏΠ΅ΡΠΈΡΠ΅ΡΡΠΉΠ½ΠΎΠ³ΠΎ ΡΠΊΠ»Π°Π΄Ρ Π»Π΅ΠΊΡΠΈΠΊΠΎ-ΡΠ΅ΠΌΠ°Π½ΡΠΈΡΠ½ΠΎΡ Π³ΡΡΠΏΠΈ.
(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 β 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
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‘ΠΈΠ½ΡΠ΅Π· ΡΠ° Π±ΡΠΎΠ»ΠΎΠ³ΡΡΠ½Π° ΠΎΡΡΠ½ΠΊΠ° [[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½-3-ΡΠ»]Π°ΡΠ΅ΡΠ°ΠΌΡΠ΄ΡΠ² Π· 1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»ΡΠ½ΠΈΠΌ ΡΠΈΠΊΠ»ΠΎΠΌ Ρ 6, 7 ΡΠ° 8 ΠΏΠΎΠ»ΠΎΠΆΠ΅Π½Π½Ρ
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.ΠΠΎΠ½Π΄Π΅Π½ΡΠΈΡΠΎΠ²Π°Π½Π½ΡΠ΅ Π³Π΅ΡΠ΅ΡΠΎΡΠΈΠΊΠ»ΠΈΡΠ΅ΡΠΊΠΈΠ΅ 1,2,4-ΡΡΠΈΠ°Π·ΠΎΠ»Ρ ΠΏΡΠΈΠ²Π»Π΅ΠΊΠ°ΡΡ Π±ΠΎΠ»ΡΡΠΎΠ΅ Π²Π½ΠΈΠΌΠ°Π½ΠΈΠ΅ ΡΠ°Π·Π½ΠΎΠΎΠ±ΡΠ°Π·ΠΈΠ΅ΠΌ ΠΈΠ½ΡΠ΅ΡΠ΅ΡΠ½ΡΡ
Π±ΠΈΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΈΡ
ΡΠ²ΠΎΠΉΡΡΠ².Π¦Π΅Π»Ρ ΡΠ°Π±ΠΎΡΡ. Π Π°Π·ΡΠ°Π±ΠΎΡΠ°ΡΡ ΠΌΠ΅ΡΠΎΠ΄ ΡΠΈΠ½ΡΠ΅Π·Π° Π½ΠΎΠ²ΡΡ
2-[(1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»-5-ΠΈΠ»)- [1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-a]ΠΏΠΈΡΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»]Π°ΡΠ΅ΡΠ°ΠΌΠΈΠ΄ΠΎΠ² ΠΈ ΠΏΡΠΎΠ²Π΅ΡΡΠΈ Π±ΠΈΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΡΡ ΠΎΡΠ΅Π½ΠΊΡ ΡΠΈΠ½ΡΠ΅Π·ΠΈΡΠΎΠ²Π°Π½Π½ΡΡ
ΡΠΎΠ΅Π΄ΠΈΠ½Π΅Π½ΠΈΠΉ.Π Π΅Π·ΡΠ»ΡΡΠ°ΡΡ ΠΈ ΠΈΡ
ΠΎΠ±ΡΡΠΆΠ΄Π΅Π½ΠΈΠ΅. Π‘ΠΈΠ½ΡΠ΅Π·ΠΈΡΠΎΠ²Π°Π½ ΡΡΠ΄ Π½ΠΎΠ²ΡΡ
ΠΏΡΠΎΠΈΠ·Π²ΠΎΠ΄Π½ΡΡ
Π°ΡΠ΅ΡΠ°ΠΌΠΈΠ΄ΠΎΠ², ΠΊΠΎΡΠΎΡΡΠΉ ΡΠΎΡΡΠΎΠΈΡ ΠΈΠ· 32 Π°Π½Π°Π»ΠΎΠ³ΠΎΠ², ΡΠΎΠ΄Π΅ΡΠΆΠ°ΡΠΈΡ
1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»ΡΠ½ΡΠΉ ΡΠΈΠΊΠ» Π² 6, 7 ΠΈ 8 ΠΏΠΎΠ»ΠΎΠΆΠ΅Π½ΠΈΡΡ
. Π£Π΄ΠΎΠ±Π½Π°Ρ ΡΡ
Π΅ΠΌΠ° ΡΠΈΠ½ΡΠ΅Π·Π° Π½Π°ΡΠΈΠ½Π°Π΅ΡΡΡ Ρ ΠΊΠΎΠΌΠΌΠ΅ΡΡΠ΅ΡΠΊΠΈ Π΄ΠΎΡΡΡΠΏΠ½ΡΡ
2-Ρ
Π»ΠΎΡΠΏΠΈΡΠΈΠ΄ΠΈΠ½-3, 2-Ρ
Π»ΠΎΡΠΏΠΈΡΠΈΠ΄ΠΈΠ½-4, 2-Ρ
Π»ΠΎΡΠΏΠΈΡΠΈΠ΄ΠΈΠ½-5-ΠΊΠ°ΡΠ±ΠΎΠ½ΠΎΠ²ΡΡ
ΠΊΠΈΡΠ»ΠΎΡ Ρ Π°ΠΌΠΈΠ΄ΠΎΠΊΡΠΈΠΌΠ°ΠΌΠΈ Ρ ΠΎΠ±ΡΠ°Π·ΠΎΠ²Π°Π½ΠΈΠ΅ΠΌ ΡΠΎΠΎΡΠ²Π΅ΡΡΡΠ²ΡΡΡΠΈΡ
2-Ρ
Π»ΠΎΡ-[3-R1-1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»-5-ΠΈΠ»]ΠΏΠΈΡΠΈΠ΄ΠΈΠ½ΠΎΠ², ΠΏΠΎΡΠ»Π΅ ΡΠ΅Π³ΠΎ ΡΠ»Π΅Π΄ΡΠ΅Ρ ΡΠ΅Π°ΠΊΡΠΈΡ Π³ΠΈΠ΄ΡΠ°Π·ΠΈΠ½ΠΎΠ»ΠΈΠ·Π° Ρ ΠΈΠ·Π±ΡΡΠΊΠΎΠΌ Π³ΠΈΠ΄ΡΠ°Π·ΠΈΠ½ Π³ΠΈΠ΄ΡΠ°ΡΠ°. ΠΡΠΎΡΠ΅ΡΡ ΠΏΡΠΎΠ΄ΠΎΠ»ΠΆΠ°Π΅ΡΡΡ ΠΏΡΡΠ΅ΠΌ ΠΎΠ±ΡΠ°Π·ΠΎΠ²Π°Π½ΠΈΡ ΡΡΠΈΡΠ° Ρ Π·Π°ΠΊΡΡΡΠΈΠ΅ΠΌ ΠΏΠΈΡΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ ΠΊΠΎΠ»ΡΡΠ°, Π·Π°ΡΠ΅ΠΌ ΡΠ΅ΡΠ΅Π· Π³ΠΈΠ΄ΡΠΎΠ»ΠΈΠ· ΠΊ ΡΠΊΡΡΡΠ½ΠΎΠΉ ΠΊΠΈΡΠ»ΠΎΡΠ΅ ΠΌΡ ΠΏΠΎΠ»ΡΡΠ°Π΅ΠΌ Π°ΠΌΠΈΠ΄Π½ΡΠ΅ ΠΎΠ±ΡΠ°Π·ΠΎΠ²Π°Π½ΠΈΡ ΠΊΠΎΠ½Π΅ΡΠ½ΡΡ
ΠΏΡΠΎΠ΄ΡΠΊΡΠΎΠ².ΠΠΊΡΠΏΠ΅ΡΠΈΠΌΠ΅Π½ΡΠ°Π»ΡΠ½Π°Ρ ΡΠ°ΡΡΡ. Π ΡΠ΄ Π½ΠΎΠ²ΡΡ
2-[6-(1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»-5-ΠΈΠ»)-, 2-[7-(1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»-5-ΠΈΠ»)-, 2-[8-(1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»-5-ΠΈΠ»)-[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°] ΠΏΠΈΡΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»]Π°ΡΠ΅ΡΠ°ΠΌΠΈΠ΄ΠΎΠ² Π±ΡΠ» ΠΏΠΎΠ»ΡΡΠ΅Π½ Ρ Ρ
ΠΎΡΠΎΡΠΈΠΌΠΈ Π²ΡΡ
ΠΎΠ΄Π°ΠΌΠΈ, Π° ΠΈΡ
ΡΡΡΡΠΊΡΡΡΡ ΠΏΠΎΠ΄ΡΠ²Π΅ΡΠΆΠ΄Π΅Π½Ρ ΠΌΠ΅ΡΠΎΠ΄ΠΎΠΌ Π―ΠΠ 1H-ΡΠΏΠ΅ΠΊΡΡΠΎΡΠΊΠΎΠΏΠΈΠΈ. Π’Π°ΠΊΠΆΠ΅ Π±ΡΠ» ΠΏΡΠΎΠ²Π΅Π΄Π΅Π½ ΠΏΡΠΎΠ³Π½ΠΎΠ· ΠΈ ΠΈΠ·ΡΡΠ΅Π½ΠΈΠ΅ ΠΈΡ
ΡΠ°ΡΠΌΠ°ΠΊΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΎΠΉ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΠΈ.ΠΡΠ²ΠΎΠ΄Ρ. Π‘ΠΈΠ½ΡΠ΅ΡΠΈΡΠ΅ΡΠΊΠΈΠΉ ΠΏΠΎΠ΄Ρ
ΠΎΠ΄ ΠΏΠΎΠ»ΡΡΠ΅Π½ΠΈΡ ΡΠ°Π½Π΅Π΅ Π½Π΅ΠΈΠ·Π²Π΅ΡΡΠ½ΡΡ
ΠΏΡΠ΅Π΄ΡΡΠ°Π²ΠΈΡΠ΅Π»Π΅ΠΉ 2-[(1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»-5-ΠΈΠ»)-[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ4,3-Π°]ΠΏΠΈΡΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»]Π°ΡΠ΅ΡΠ°ΠΌΠΈΠ΄ΠΎΠ² ΠΌΠΎΠΆΠ΅Ρ Π±ΡΡΡ ΠΏΡΠΈΠΌΠ΅Π½Π΅Π½ Π΄Π»Ρ ΡΠΈΠ½ΡΠ΅Π·Π° ΡΠ°Π·Π»ΠΈΡΠ½ΡΡ
ΡΡΠ½ΠΊΡΠΈΠΎΠ½Π°Π»ΠΈΠ·ΠΈΡΠΎΠ²Π°Π½Π½ΡΡ
[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡΠΈΠ΄ΠΈΠ½ΠΎΠ²ΡΡ
ΠΏΡΠΎΠΈΠ·Π²ΠΎΠ΄Π½ΡΡ
.ΠΠΎΠ½Π΄Π΅Π½ΡΠΎΠ²Π°Π½Ρ Π³Π΅ΡΠ΅ΡΠΎΡΠΈΠΊΠ»ΡΡΠ½Ρ 1,2,4-ΡΡΠΈΠ°Π·ΠΎΠ»ΠΈ ΠΏΡΠΈΠ²Π΅ΡΡΠ°ΡΡΡ Π²Π΅Π»ΠΈΠΊΡ ΡΠ²Π°Π³Ρ Π΄ΠΎ ΡΠ΅Π±Π΅ ΡΡΠ·Π½ΠΎΠΌΠ°Π½ΡΡΠ½ΡΡΡΡ ΡΡΠΊΠ°Π²ΠΈΡ
Π±ΡΠΎΠ»ΠΎΠ³ΡΡΠ½ΠΈΡ
Π²Π»Π°ΡΡΠΈΠ²ΠΎΡΡΠ΅ΠΉ.ΠΠ΅ΡΠ° ΡΠΎΠ±ΠΎΡΠΈ. Π ΠΎΠ·ΡΠΎΠ±ΠΈΡΠΈ ΠΌΠ΅ΡΠΎΠ΄ ΡΠΈΠ½ΡΠ΅Π·Ρ Π½ΠΎΠ²ΠΈΡ
2-[(1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»-5-ΡΠ»)-[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½-3-ΡΠ»]Π°ΡΠ΅ΡΠ°ΠΌΡΠ΄ΡΠ² ΡΠ° ΠΏΡΠΎΠ²Π΅ΡΡΠΈ Π±ΡΠΎΠ»ΠΎΠ³ΡΡΠ½Ρ ΠΎΡΡΠ½ΠΊΡ ΡΠΈΠ½ΡΠ΅Π·ΠΎΠ²Π°Π½ΠΈΡ
ΡΠΏΠΎΠ»ΡΠΊ.Π Π΅Π·ΡΠ»ΡΡΠ°ΡΠΈ ΡΠ° ΡΡ
ΠΎΠ±Π³ΠΎΠ²ΠΎΡΠ΅Π½Π½Ρ. Π‘ΠΈΠ½ΡΠ΅Π·ΠΎΠ²Π°Π½ΠΎ Π½ΠΈΠ·ΠΊΡ Π½ΠΎΠ²ΠΈΡ
ΠΏΠΎΡ
ΡΠ΄Π½ΠΈΡ
Π°ΡΠ΅ΡΠ°ΠΌΡΠ΄ΡΠ², ΡΠΊΠ° ΡΠΊΠ»Π°Π΄Π°ΡΡΡΡΡ Π· 32 Π°Π½Π°Π»ΠΎΠ³ΡΠ², ΡΠΎ ΠΌΡΡΡΡΡΡ 1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»ΡΠ½ΠΈΠΉ ΡΠΈΠΊΠ» Ρ 6, 7 ΡΠ° 8 ΠΏΠΎΠ»ΠΎΠΆΠ΅Π½Π½ΡΡ
. ΠΡΡΡΠ½Π° ΡΡ
Π΅ΠΌΠ° ΡΠΈΠ½ΡΠ΅Π·Ρ ΠΏΠΎΡΠΈΠ½Π°ΡΡΡΡΡ Π· ΠΊΠΎΠΌΠ΅ΡΡΡΠΉΠ½ΠΎ Π΄ΠΎΡΡΡΠΏΠ½ΠΈΡ
2-Ρ
Π»ΠΎΡΠΎΠΏΡΡΠΈΠ΄ΠΈΠ½-3-, 2-Ρ
Π»ΠΎΡΠΎΠΏΡΡΠΈΠ΄ΠΈΠ½-4-, 2-Ρ
Π»ΠΎΡΠΎΠΏΡΡΠΈΠ΄ΠΈΠ½-5-ΠΊΠ°ΡΠ±ΠΎΠ½ΠΎΠ²ΠΈΡ
ΠΊΠΈΡΠ»ΠΎΡ Π· Π°ΠΌΡΠ΄ΠΎΠΊΡΠΈΠΌΠ°ΠΌΠΈ Π· ΡΡΠ²ΠΎΡΠ΅Π½Π½ΡΠΌ Π²ΡΠ΄ΠΏΠΎΠ²ΡΠ΄Π½ΠΈΡ
2-Ρ
Π»ΠΎΡΠΎ-[3-R1-1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»-5-ΡΠ»]ΠΏΡΡΠΈΠ΄ΠΈΠ½ΡΠ², ΠΏΡΡΠ»Ρ ΡΠΎΠ³ΠΎ ΠΏΠ΅ΡΠ΅Π±ΡΠ³Π°Ρ ΡΠ΅Π°ΠΊΡΡΡ Π³ΡΠ΄ΡΠ°Π·ΠΈΠ½ΠΎΠ»ΡΠ·Ρ Π· Π½Π°Π΄Π»ΠΈΡΠΊΠΎΠΌ Π³ΡΠ΄ΡΠ°Π·ΠΈΠ½ Π³ΡΠ΄ΡΠ°ΡΡ. ΠΡΠΎΡΠ΅Ρ ΠΏΡΠΎΠ΄ΠΎΠ²ΠΆΡΡΡΡΡΡ ΡΠ»ΡΡ
ΠΎΠΌ ΡΡΠ²ΠΎΡΠ΅Π½Π½Ρ Π΅ΡΡΡΡ Π· Π·Π°ΠΊΡΠΈΡΡΡΠΌ ΠΏΡΡΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ ΠΊΡΠ»ΡΡΡ, ΠΏΠΎΡΡΠΌ ΡΠ΅ΡΠ΅Π· Π³ΡΠ΄ΡΠΎΠ»ΡΠ· Π΄ΠΎ ΠΎΡΡΠΎΠ²ΠΎΡ ΠΊΠΈΡΠ»ΠΎΡΠΈ ΠΌΠΈ ΠΎΡΡΠΈΠΌΡΡΠΌΠΎ Π°ΠΌΡΠ΄Π½Ρ ΡΡΠ²ΠΎΡΠ΅Π½Π½Ρ ΠΊΡΠ½ΡΠ΅Π²ΠΈΡ
ΠΏΡΠΎΠ΄ΡΠΊΡΡΠ².ΠΠΊΡΠΏΠ΅ΡΠΈΠΌΠ΅Π½ΡΠ°Π»ΡΠ½Π° ΡΠ°ΡΡΠΈΠ½Π°. Π ΡΠ΄ Π½ΠΎΠ²ΠΈΡ
2-[6-(1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»-5-ΡΠ»)-, 2-[7-(1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»-5-ΡΠ»)-, 2-[8-(1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»-5-ΡΠ»)-[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½-3-ΡΠ»]Π°ΡΠ΅ΡΠ°ΠΌΡΠ΄ΡΠ² Π±ΡΠ² ΠΎΡΡΠΈΠΌΠ°Π½ΠΈΠΉ Π· Π΄ΠΎΠ±ΡΠΈΠΌΠΈ Π²ΠΈΡ
ΠΎΠ΄Π°ΠΌΠΈ, Π° ΡΡ
ΡΡΡΡΠΊΡΡΡΠΈ ΠΏΡΠ΄ΡΠ²Π΅ΡΠ΄ΠΆΠ΅Π½Ρ ΠΌΠ΅ΡΠΎΠ΄ΠΎΠΌ Π―ΠΠ 1H-ΡΠΏΠ΅ΠΊΡΡΠΎΡΠΊΠΎΠΏΡΡ. Π’Π°ΠΊΠΎΠΆ Π±ΡΠ»ΠΎ Π·ΡΠΎΠ±Π»Π΅Π½ΠΎ ΠΏΡΠΎΠ³Π½ΠΎΠ· ΡΠ° Π²ΠΈΠ²ΡΠ΅Π½Π½Ρ ΡΡ
ΡΠ°ΡΠΌΠ°ΠΊΠΎΠ»ΠΎΠ³ΡΡΠ½ΠΎΡ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΡ.ΠΠΈΡΠ½ΠΎΠ²ΠΊΠΈ. Π‘ΠΈΠ½ΡΠ΅ΡΠΈΡΠ½ΠΈΠΉ ΠΏΡΠ΄Ρ
ΡΠ΄ Π΄ΠΎ ΠΎΡΡΠΈΠΌΠ°Π½Π½Ρ ΡΠ°Π½ΡΡΠ΅ Π½Π΅Π²ΡΠ΄ΠΎΠΌΠΈΡ
ΠΏΡΠ΅Π΄ΡΡΠ°Π²Π½ΠΈΠΊΡΠ² 2-[(1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»-5-ΡΠ»)-[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½-3-ΡΠ»]Π°ΡΠ΅ΡΠ°ΠΌΡΠ΄ΡΠ² ΠΌΠΎΠΆΠ΅ Π±ΡΡΠΈ Π·Π°ΡΡΠΎΡΠΎΠ²Π°Π½ΠΈΠΉ Π΄Π»Ρ ΡΠΈΠ½ΡΠ΅Π·Ρ ΡΡΠ·Π½ΠΎΠΌΠ°Π½ΡΡΠ½ΠΈΡ
ΡΡΠ½ΠΊΡΡΠΎΠ½Π°Π»ΡΠ·ΠΎΠ²Π°Π½ΠΈΡ
[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΈΡ
ΠΏΠΎΡ
ΡΠ΄Π½ΠΈΡ
EPIDEMIOLOGICAL MANIFESTATIONS OF PREVALENCE OF GLOMERULAR-TUBULOINTERSTITIAL DISEASES OF KIDNEYS AND URETER IN AREAS WITH DIFFERENT LEVELS OF ANTHROPOGENIC LOAD
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‘ΡΠ΅Π΄ΠΈ ΠΈΠ·ΡΡΠ°Π΅ΠΌΡΡ
ΡΠ΅ΡΡΠΈΡΠΎΡΠΈΠΉ Π½Π°ΠΈΠΌΠ΅Π½ΡΡΠ΅Π΅ Π½Π΅Π±Π»Π°Π³ΠΎΠΏΠΎΠ»ΡΡΠΈΠ΅ ΠΏΠΎ Π²ΡΡΠ°ΠΆΠ΅Π½Π½ΠΎΡΡΠΈ ΠΏΡΠ΅Π²Π°Π»Π΅Π½ΡΠ½ΠΎΡΡΠΈ 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
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
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-1Ξ², IL-6, IL-8, Π€ΠΠ-Ξ± 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
ΠΠΎΡΡΠΊ Π½ΠΎΠ²ΠΈΡ ΠΏΠΎΡΠ΅Π½ΡΡΠΉΠ½ΠΈΡ ΡΠ½Π³ΡΠ±ΡΡΠΎΡΡΠ² ΠΏΡΠΎΡΠ΅ΡΠ½ΠΊΡΠ½Π°Π·ΠΈ Pim-1 ΡΠ΅ΡΠ΅Π΄ Π°ΠΌΡΠ΄ΡΠ² 1,2,4-ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½-3-ΠΌΠ΅ΡΠ°Π½Π°ΠΌΡΠ½Ρ Π· 1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»ΡΠ½ΠΈΠΌ ΡΠΈΠΊΠ»ΠΎΠΌ Ρ 7 ΡΠ° 8 ΠΏΠΎΠ»ΠΎΠΆΠ΅Π½Π½ΡΡ
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΅ΡΠΌΠ΅Π½Ρ Pim-1 ΠΈΠ· ΡΠ΅ΠΌΠ΅ΠΉΡΡΠ²Π° ΡΠ΅ΡΠΈΠ½/ΡΡΠ΅ΠΎΠ½ΠΈΠ½ ΠΏΡΠΎΡΠ΅ΠΈΠ½ΠΊΠΈΠ½Π°Π·Ρ ΡΠ²Π»ΡΠ΅ΡΡΡ Π²Π΅ΡΠΎΡΡΠ½ΠΎΠΉ ΠΌΠΈΡΠ΅Π½ΡΡ Π΄Π»Ρ ΡΠ°ΡΠ³Π΅ΡΠ½ΠΎΠΉ ΡΠ΅ΡΠ°ΠΏΠΈΠΈ ΠΎΠΏΡΡ
ΠΎΠ»Π΅ΠΉ ΠΊΡΠΎΠ²Π΅ΡΠ²ΠΎΡΠ½ΠΎΠΉ ΠΈ Π»ΠΈΠΌΡΠΎΠΈΠ΄Π½ΠΎΠΉ ΡΠΊΠ°Π½Π΅ΠΉ. Π’ΡΠΈΠ°Π·ΠΎΠ»ΠΎΠΏΠΈΡΠΈΠ΄ΠΈΠ½Ρ β ΡΡΠΎ ΡΠ½ΠΈΠ²Π΅ΡΡΠ°Π»ΡΠ½ΡΠΉ ΡΠΊΠ°ΡΡΠΎΠ»Π΄, Π½Π° Π±Π°Π·Π΅ ΠΊΠΎΡΠΎΡΠΎΠ³ΠΎ ΠΏΡΠΎΠ²ΠΎΠ΄ΡΡΡΡ ΠΌΠ΅ΠΆΠ΄ΡΠ½Π°ΡΠΎΠ΄Π½ΡΠ΅ Π½Π°ΡΡΠ½ΡΠ΅ ΠΏΡΠΎΠ³ΡΠ°ΠΌΠΌΡ ΠΏΠΎ ΡΠ°Π·ΡΠ°Π±ΠΎΡΠΊΠ΅ ΠΏΠΎΡΠ΅Π½ΡΠΈΠ°Π»ΡΠ½ΡΡ
ΠΏΡΠΎΡΠΈΠ²ΠΎΡΠ°ΠΊΠΎΠ²ΡΡ
ΡΡΠ΅Π΄ΡΡΠ².Π¦Π΅Π»Ρ. Π‘ΠΎΠ·Π΄Π°ΡΡ ΡΠ°ΡΠΌΠ°ΠΊΠΎΡΠΎΡΠ½ΡΡ ΠΌΠΎΠ΄Π΅Π»Ρ Π΄Π»Ρ ΠΏΠΎΠΈΡΠΊΠ° Π½ΠΎΠ²ΡΡ
ΠΏΠΎΡΠ΅Π½ΡΠΈΠ°Π»ΡΠ½ΡΡ
ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΠΎΠ² Pim-1. ΠΡΠΎΠ²Π΅ΡΡΠΈ Π²ΠΈΡΡΡΠ°Π»ΡΠ½ΡΠΉ ΡΠΊΡΠΈΠ½ΠΈΠ½Π³ ΡΠΌΠΎΠ΄Π΅Π»ΠΈΡΠΎΠ²Π°Π½Π½ΠΎΠΉ Π±Π°Π·Ρ Π½ΠΎΠ²ΡΡ
ΠΏΡΠΎΠΈΠ·Π²ΠΎΠ΄Π½ΡΡ
1,2,4-ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡΠΈΠ΄ΠΈΠ½ΠΎΠ² ΠΈ ΡΠ°Π·ΡΠ°Π±ΠΎΡΠ°ΡΡ ΠΌΠ΅ΡΠΎΠ΄ ΡΠΈΠ½ΡΠ΅Π·Π° Π°ΠΌΠΈΠ΄ΠΎΠ² 1,2,4-ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡΠΈΠ΄ΠΈΠ½-3-ΠΌΠ΅ΡΠ°Π½Π°ΠΌΠΈΠ½Π°, ΡΠΎΠ΄Π΅ΡΠΆΠ°ΡΠΈΡ
1,2,4-ΠΈΠ·ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»ΡΠ½ΡΠΉ ΡΠΈΠΊΠ».Π Π΅Π·ΡΠ»ΡΡΠ°ΡΡ ΠΈ ΠΎΠ±ΡΡΠΆΠ΄Π΅Π½ΠΈΠ΅. Π‘ΠΎΠ·Π΄Π°Π½Π° ΠΈ Π²Π°Π»ΠΈΠ΄ΠΈΡΠΎΠ²Π°Π½Π° ΡΠ°ΡΠΌΠ°ΠΊΠΎΡΠΎΡΠ½Π°Ρ ΠΌΠΎΠ΄Π΅Π»Ρ ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΠΎΠ² Pim-1 Π½Π° ΠΎΡΠ½ΠΎΠ²Π΅ ΠΈΠ·Π²Π΅ΡΡΠ½ΠΎΠΉ ΠΈΠ½ΡΠΎΡΠΌΠ°ΡΠΈΠΈ ΠΎ ΡΡΡΡΠΊΡΡΡΠ°Ρ
Π°ΠΊΡΠΈΠ²Π½ΡΡ
Π»ΠΈΠ³Π°Π½Π΄ΠΎΠ². ΠΡΠΎΠ²Π΅Π΄Π΅Π½ Π²ΠΈΡΡΡΠ°Π»ΡΠ½ΡΠΉ ΡΠΊΡΠΈΠ½ΠΈΠ½Π³ Π±ΠΈΠ±Π»ΠΈΠΎΡΠ΅ΠΊΠΈ ΠΈΠ· 912 ΡΠΎΠ΅Π΄ΠΈΠ½Π΅Π½ΠΈΠΉ, ΡΠ΅Π·ΡΠ»ΡΡΠ°ΡΠΎΠΌ ΠΊΠΎΡΠΎΡΠΎΠ³ΠΎ ΡΡΠ°Π» ΡΠΏΠΈΡΠΎΠΊ Ρ
ΠΈΡΠΎΠ² ΠΈΠ· 175 ΡΠΎΠ΅Π΄ΠΈΠ½Π΅Π½ΠΈΠΉ. ΠΠ»Ρ ΡΠΈΠ½ΡΠ΅Π·Π° Π±ΡΠ»ΠΈ ΠΎΡΠΎΠ±ΡΠ°Π½Ρ 15 ΡΠΎΠ΅Π΄ΠΈΠ½Π΅Π½ΠΈΠΉ Ρ Π½Π°ΠΈΠ±ΠΎΠ»Π΅Π΅ Π²ΡΡΠΎΠΊΠΎΠΉ ΡΠ°ΡΠΌΠ°ΠΊΠΎΡΠΎΡΠ½ΠΎΠΉ ΠΎΡΠ΅Π½ΠΊΠΎΠΉ. Π‘ΠΈΠ½ΡΠ΅Π·ΠΈΡΠΎΠ²Π°Π½Ρ 15 ΡΠΎΠ΅Π΄ΠΈΠ½Π΅Π½ΠΈΠΉ, ΡΠ²Π»ΡΡΡΠΈΡ
ΡΡ ΠΏΠΎΡΠ΅Π½ΡΠΈΠ°Π»ΡΠ½ΡΠΌΠΈ ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΠ°ΠΌΠΈ ΠΊΠΈΠ½Π°Π·Ρ Pim-1.ΠΠΊΡΠΏΠ΅ΡΠΈΠΌΠ΅Π½ΡΠ°Π»ΡΠ½Π°Ρ ΡΠ°ΡΡΡ. Π Π°Π·ΡΠ°Π±ΠΎΡΠ°Π½Π° ΡΡ
Π΅ΠΌΠ°, ΠΌΠ΅ΡΠΎΠ΄ΠΈΠΊΠΈ ΡΠΈΠ½ΡΠ΅Π·Π° ΠΈ ΡΠΈΠ½ΡΠ΅Π·ΠΈΡΠΎΠ²Π°Π½Ρ ΡΠΈΡΡΠ΅ΠΌΠ°ΡΠΈΡΠ΅ΡΠΊΠΈΠ΅ ΡΡΠ΄Ρ Π½ΠΎΠ²ΡΡ
Π°ΠΌΠΈΠ΄ΠΎΠ² (7-(1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»-5-ΠΈΠ»)-[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»)ΠΌΠ΅ΡΠ°Π½Π°ΠΌΠΈΠ½Π° ΠΈ (8-(1,2,4-ΠΎΠΊΡΠ°Π΄ΠΈΠ°Π·ΠΎΠ»-5-ΠΈΠ»)-[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΠΈΡΠΈΠ΄ΠΈΠ½-3-ΠΈΠ»)ΠΌΠ΅ΡΠ°Π½Π°ΠΌΠΈΠ½Π°.ΠΡΠ²ΠΎΠ΄Ρ. ΠΠΎΠ»ΡΡΠ΅Π½Π½ΡΠ΅ ΡΠΎΠ΅Π΄ΠΈΠ½Π΅Π½ΠΈΡ ΡΠ²Π»ΡΡΡΡΡ ΠΏΠΎΡΠ΅Π½ΡΠΈΠ°Π»ΡΠ½ΡΠΌΠΈ ΠΈΠ½Π³ΠΈΠ±ΠΈΡΠΎΡΠ°ΠΌΠΈ ΠΊΠΈΠ½Π°Π·Ρ Pim-1. ΠΠ°Π»ΡΠ½Π΅ΠΉΡΠΈΠ΅ ΠΈΡΡΠ»Π΅Π΄ΠΎΠ²Π°Π½ΠΈΡ Π±ΡΠ΄ΡΡ Π½Π°ΠΏΡΠ°Π²Π»Π΅Π½Ρ Π½Π° Π²ΡΡΠ²Π»Π΅Π½ΠΈΠ΅ ΠΏΡΠΎΡΠΈΠ²ΠΎΠΎΠΏΡΡ
ΠΎΠ»Π΅Π²ΠΎΠΉ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΠΈ ΡΠΈΠ½ΡΠ΅Π·ΠΈΡΠΎΠ²Π°Π½Π½ΡΡ
ΡΠΎΠ΅Π΄ΠΈΠ½Π΅Π½ΠΈΠΉ ΠΌΠ΅ΡΠΎΠ΄Π°ΠΌΠΈ in vitro ΠΈ in vivo.Π€Π΅ΡΠΌΠ΅Π½Ρ Pim-1 Π· ΡΡΠΌΠ΅ΠΉΡΡΠ²Π° ΡΠ΅ΡΠΈΠ½/ΡΡΠ΅ΠΎΠ½ΡΠ½ ΠΏΡΠΎΡΠ΅ΡΠ½ΠΊΡΠ½Π°Π· Ρ ΠΉΠΌΠΎΠ²ΡΡΠ½ΠΎΡ ΠΌΡΡΠ΅Π½Π½Ρ Π΄Π»Ρ ΡΠ°ΡΠ³Π΅ΡΠ½ΠΎΡ ΡΠ΅ΡΠ°ΠΏΡΡ ΠΏΡΡ
Π»ΠΈΠ½ ΠΊΡΠΎΠ²ΠΎΡΠ²ΠΎΡΠ½ΠΎΡ ΡΠ° Π»ΡΠΌΡΠΎΡΠ΄Π½ΠΎΡ ΡΠΊΠ°Π½ΠΈΠ½ΠΈ. Π’ΡΠΈΠ°Π·ΠΎΠ»ΠΎΠΏΡΡΠΈΠ΄ΠΈΠ½ΠΈ β ΡΠ΅ ΡΠ½ΡΠ²Π΅ΡΡΠ°Π»ΡΠ½ΠΈΠΉ ΡΠΊΠ°ΡΠΎΠ»Π΄, Π½Π° Π±Π°Π·Ρ ΡΠΊΠΎΠ³ΠΎ ΡΠ΅Π°Π»ΡΠ·ΡΡΡΡΡΡ ΠΌΡΠΆΠ½Π°ΡΠΎΠ΄Π½Ρ Π½Π°ΡΠΊΠΎΠ²Ρ ΠΏΡΠΎΠ³ΡΠ°ΠΌΠΈ Π· ΡΠΎΠ·ΡΠΎΠ±ΠΊΠΈ ΠΏΠΎΡΠ΅Π½ΡΡΠΉΠ½ΠΈΡ
ΠΏΡΠΎΡΠΈΡΠ°ΠΊΠΎΠ²ΠΈΡ
Π·Π°ΡΠΎΠ±ΡΠ².ΠΠ΅ΡΠ°. Π‘ΡΠ²ΠΎΡΠΈΡΠΈ ΡΠ°ΡΠΌΠ°ΠΊΠΎΡΠΎΡΠ½Ρ ΠΌΠΎΠ΄Π΅Π»Ρ Π΄Π»Ρ ΠΏΠΎΡΡΠΊΡ Π½ΠΎΠ²ΠΈΡ
ΠΏΠΎΡΠ΅Π½ΡΡΠΉΠ½ΠΈΡ
ΡΠ½Π³ΡΠ±ΡΡΠΎΡΡΠ² Pim-1. ΠΡΠΎΠ²Π΅ΡΡΠΈ Π²ΡΡΡΡΠ°Π»ΡΠ½ΠΈΠΉ ΡΠΊΡΠΈΠ½ΡΠ½Π³ Π·ΠΌΠΎΠ΄Π΅Π»ΡΠΎΠ²Π°Π½ΠΎΡ Π±Π°Π·ΠΈ Π½ΠΎΠ²ΠΈΡ
ΠΏΠΎΡ
ΡΠ΄Π½ΠΈΡ
1,2,4-ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½Ρ ΡΠ° ΡΠΎΠ·ΡΠΎΠ±ΠΈΡΠΈ ΠΌΠ΅ΡΠΎΠ΄ ΡΠΈΠ½ΡΠ΅Π·Ρ Π°ΠΌΡΠ΄ΡΠ² 1,2,4-ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½-3-ΠΌΠ΅ΡΠ°Π½Π°ΠΌΡΠ½Ρ, ΡΠΎ ΠΌΡΡΡΡΡΡ 1,2,4-ΡΠ·ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»ΡΠ½ΠΈΠΉ ΡΠΈΠΊΠ».Π Π΅Π·ΡΠ»ΡΡΠ°ΡΠΈ ΡΠ° ΠΎΠ±Π³ΠΎΠ²ΠΎΡΠ΅Π½Π½Ρ. Π‘ΡΠ²ΠΎΡΠ΅Π½ΠΎ ΡΠ° Π²Π°Π»ΡΠ΄ΠΎΠ²Π°Π½ΠΎ ΡΠ°ΡΠΌΠ°ΠΊΠΎΡΠΎΡΠ½Ρ ΠΌΠΎΠ΄Π΅Π»Ρ ΡΠ½Π³ΡΠ±ΡΡΠΎΡΡΠ² Pim-1 Π½Π° ΠΎΡΠ½ΠΎΠ²Ρ Π²ΡΠ΄ΠΎΠΌΠΎΡ ΡΠ½ΡΠΎΡΠΌΠ°ΡΡΡ ΠΏΡΠΎ ΡΡΡΡΠΊΡΡΡΠΈ Π°ΠΊΡΠΈΠ²Π½ΠΈΡ
Π»ΡΠ³Π°Π½Π΄ΡΠ². ΠΡΠΎΠ²Π΅Π΄Π΅Π½ΠΎ Π²ΡΡΡΡΠ°Π»ΡΠ½ΠΈΠΉ ΡΠΊΡΠΈΠ½ΡΠ½Π³ Π±ΡΠ±Π»ΡΠΎΡΠ΅ΠΊΠΈ Π· 912 ΡΠΏΠΎΠ»ΡΠΊ, ΡΠ΅Π·ΡΠ»ΡΡΠ°ΡΠΎΠΌ ΡΠΊΠΎΠ³ΠΎ ΡΡΠ°Π² ΡΠΏΠΈΡΠΎΠΊ Ρ
ΡΡΡΠ² ΡΠ· 175 ΡΠΏΠΎΠ»ΡΠΊ. ΠΠ»Ρ ΡΠΈΠ½ΡΠ΅Π·Ρ Π±ΡΠ»ΠΎ Π²ΡΠ΄ΡΠ±ΡΠ°Π½ΠΎ 15 ΡΠΏΠΎΠ»ΡΠΊ Π· Π½Π°ΠΉΠ²ΠΈΡΠΎΡ ΡΠ°ΡΠΌΠ°ΠΊΠΎΡΠΎΡΠ½ΠΎΡ ΠΎΡΡΠ½ΠΊΠΎΡ. Π‘ΠΈΠ½ΡΠ΅Π·ΠΎΠ²Π°Π½ΠΎ 15 ΡΠΏΠΎΠ»ΡΠΊ, ΡΠΎ Ρ ΠΏΠΎΡΠ΅Π½ΡΡΠΉΠ½ΠΈΠΌΠΈ ΡΠ½Π³ΡΠ±ΡΡΠΎΡΠ°ΠΌΠΈ ΠΊΡΠ½Π°Π·ΠΈ Pim-1.ΠΠΊΡΠΏΠ΅ΡΠΈΠΌΠ΅Π½ΡΠ°Π»ΡΠ½Π° ΡΠ°ΡΡΠΈΠ½Π°. Π ΠΎΠ·ΡΠΎΠ±Π»Π΅Π½ΠΎ ΡΡ
Π΅ΠΌΡ, ΠΌΠ΅ΡΠΎΠ΄ΠΈΠΊΠΈ ΡΠΈΠ½ΡΠ΅Π·Ρ ΡΠ° ΡΠΈΠ½ΡΠ΅Π·ΠΎΠ²Π°Π½ΠΎ ΡΠΈΡΡΠ΅ΠΌΠ°ΡΠΈΡΠ½Ρ ΡΡΠ΄ΠΈ Π½ΠΎΠ²ΠΈΡ
Π°ΠΌΡΠ΄ΡΠ² (7-(1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»-5-ΡΠ»)-[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½-3-ΡΠ»)ΠΌΠ΅ΡΠ°Π½Π°ΠΌΡΠ½Ρ ΡΠ° (8-(1,2,4-ΠΎΠΊΡΠ°Π΄ΡΠ°Π·ΠΎΠ»-5-ΡΠ»)-[1,2,4]ΡΡΠΈΠ°Π·ΠΎΠ»ΠΎ[4,3-Π°]ΠΏΡΡΠΈΠ΄ΠΈΠ½-3-ΡΠ»)ΠΌΠ΅ΡΠ°Π½Π°ΠΌΡΠ½Ρ.ΠΠΈΡΠ½ΠΎΠ²ΠΊΠΈ. ΠΡΡΠΈΠΌΠ°Π½Ρ ΡΠΏΠΎΠ»ΡΠΊΠΈ Ρ ΠΏΠΎΡΠ΅Π½ΡΡΠΉΠ½ΠΈΠΌΠΈ ΡΠ½Π³ΡΠ±ΡΡΠΎΡΠ°ΠΌΠΈ ΠΊΡΠ½Π°Π·ΠΈ Pim-1. ΠΠΎΠ΄Π°Π»ΡΡΡ Π΄ΠΎΡΠ»ΡΠ΄ΠΆΠ΅Π½Π½Ρ Π±ΡΠ΄ΡΡΡ ΡΠΏΡΡΠΌΠΎΠ²Π°Π½Ρ Π½Π° Π²ΠΈΡΠ²Π»Π΅Π½Π½Ρ ΠΏΡΠΎΡΠΈΠΏΡΡ
Π»ΠΈΠ½Π½ΠΎΡ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΡ ΡΠΈΠ½ΡΠ΅Π·ΠΎΠ²Π°Π½ΠΈΡ
ΡΠΏΠΎΠ»ΡΠΊ ΠΌΠ΅ΡΠΎΠ΄Π°ΠΌΠΈ in vitro ΡΠ° in vivo
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