A series of N-acyl derivatives of anabasine and cytisine were prepared, to discover novel, natural product-based medicinal agents. All synthesized compounds were tested for antimicrobial, antifungal, ...antiviral and analgesic activity. The most pronounced antibacterial activity was shown by the compounds with isoxazole fragments, while the adamantane derivatives showed the greatest antiviral effect. It was found that the majority of anabasine derivatives showed significant analgesic activity, reducing the pain response of animals to the irritating effect of acetic acid. The presence of a high level of antimicrobial and antiviral activity in newly synthesized compounds makes it possible to consider them promising for further study of their pharmacological properties.
Alkaloid-based urea derivatives were produced with high yield through the reaction of anabasine and cytisine with isoxazolylphenylcarbamates in boiling benzene. Their antitumor activity, in ...combination with the commonly used five anticancer drugs, namely cyclophosphane, fluorouracil, etoposide, cisplatin, ribomustine with different mechanisms of action, was investigated. Based on the quantum chemical calculations data and molecular docking, hypotheses have been put forward to explain their mutual influence when affecting C6 rat glioma model cells.
An efficient method of producing quinine derivatives via reaction of acylation with 4,5-dichloroisothiazole-3-, 5-arylisoxazole-3-, adamantane- and hydrochlorides of pyridine-3- and ...pyridine-4-carbonyl chlorides was developed. All synthesized compounds were tested for antiviral, antimicrobial and analgesic activity. The most pronounced antibacterial activity was shown by the compounds
,
,
and
with isoxazole and pyridine fragments. It was found that most of the tested compounds showed significant analgesic activity reducing the pain response of animals to the irritating effect of acetic acid.
The title compound, C
H
N
OS, crystallizes with two independent mol-ecules in the asymmetric unit. In the crystal, the N-H⋯N and C-H⋯N hydrogen bonds connect the mol-ecules, generating double layers ...parallel to the (001) plane. The layers are joined by C-H⋯π inter-actions to form a three-dimensional supra-molecular structure.
The title compound, C
11
H
8
N
4
OS, crystallizes with two independent molecules in the asymmetric unit. In the crystal, the N—H...N and C—H...N hydrogen bonds connect the molecules, generating ...double layers parallel to the (001) plane. The layers are joined by C—H...π interactions to form a three-dimensional supramolecular structure.
2-Mercapto-1,3,4-triazoles and 2-amino-1,3,4-thiadiazoles were synthesized by successive transformations of 5-arylisoxazole- and 4,5-dichloroisothiazole-3-carboxylic acids and their derivatives. The ...amino group of 5-(4,5-dichloroisothiazol-3-yl)-1,3,4-thiadiazol-2-amine was acylated with 5-phenylisoxazole-3-carboxylic acid chloride. Simple approaches to the preparation of previously unknown heterocyclic assemblies containing two or three azole rings with a high potential for biological activity are described.
A series of N-acyl derivatives of anabasine and cytisine were prepared, to discover novel, natural product-based medicinal agents. All synthesized compounds were tested for antimicrobial, antifungal, ...antiviral and analgesic activity. The most pronounced antibacterial activity was shown by the compounds with isoxazole fragments, while the adamantane derivatives showed the greatest antiviral effect. It was found that the majority of anabasine derivatives showed significant analgesic activity, reducing the pain response of animals to the irritating effect of acetic acid. The presence of a high level of antimicrobial and antiviral activity in newly synthesized compounds makes it possible to consider them promising for further study of their pharmacological properties.
Background. New challenges of the time require the actualization of cultural codes that ensure the stability of Russian world. Special attention is to be paid to education of the younger generations ...as bearers of traditional Russian values. The appeal to national musical culture meets the priorities of the state policy, reflected in the Decree of the President of the Russian Federation dated November 9, 2022 No. 809. Objective. The aim is to analyze the potential of Russian music of the 2nd half of the 20th century in introducing students to traditional Russian values and the peculiarities of its perception by modern schoolchildren. Results. The analysis of educational programmes and of the repertoire of music education in different types of educational organizations showed the need to introduce students to the national musical culture through perception of Russian music of the 2nd half of the 20th century. The educational potential of modern local musical works is revealed in the interiorization of traditional Russian values by students. Approaches to the design of programmes as well as to the selection of the repertoire for music education are developed. Conclusions. New challenges of the time create the need to update music education programmes in order to deepen students' acquaintance with the national musical culture. The perception of musical works should take place in both the historical and cultural and the modern context. Musical culture is a holistic phenomenon, a diverse hierarchical system of relations, including philosophical, aesthetic, and ethical foundations of the value attitude to musical art in various types of musical and creative activities. To make continuous musical education effective, it is necessary to appeal to modern musical culture. Immersion of students in the musical continuum of modern culture creates conditions in which not only the musical and creative development of students takes place more organically, but also the formation of the qualities of a true “man of culture”, spirituality, morality, and patriotism are developed. The basis of musical perception is the ability to hear and experience musical content as an artistic and figurative reflection of reality, which determines its powerful influence on personality. Music is designed to develop a sense of inner involvement in the spiritual culture of the native country.
El artículo analiza dibujos decorativos enviados al Concurso de Dibujo de toda Rusia entre estudiantes de organizaciones de educación general por el 500 aniversario del Tula Kremlin (Tula, Rusia) ...sobre el tema "Tula Kremlin es el orgullo de Rusia". La relevancia de estudiar la solución decorativa de los dibujos infantiles está asociada con el hecho de que el dibujo decorativo refleja más plenamente el deseo del niño de expresar su actitud emocional ante la realidad. El artículo analiza el efecto decorativo de los dibujos infantiles en temas históricos; clasifica dibujos competitivos; considera técnicas artísticas que ayudan a dirigir la búsqueda creativa de un estudiante en el camino del desarrollo artístico emocional
The article analyzes decorative drawings sent to the All-Russian Drawing Competition among students of general education organizations for the 500th anniversary of the Tula Kremlin (Tula, Russia) on ...the topic "Tula Kremlin is the pride of Russia". The relevance of studying the decorative solution of children's drawings is associated with the fact that decorative drawing most fully reflects the child's desire to express their emotional attitude to reality. The article analyzes the decorative effect of children's drawings on historical themes; classifies competitive drawings; considers artistic techniques that help to direct the creative search of a student on the path of emotional artistic development.
El artículo analiza dibujos decorativos enviados al Concurso de Dibujo de toda Rusia entre estudiantes de organizaciones de educación general por el 500 aniversario del Tula Kremlin (Tula, Rusia) sobre el tema "Tula Kremlin es el orgullo de Rusia". La relevancia de estudiar la solución decorativa de los dibujos infantiles está asociada con el hecho de que el dibujo decorativo refleja más plenamente el deseo del niño de expresar su actitud emocional ante la realidad. El artículo analiza el efecto decorativo de los dibujos infantiles en temas históricos; clasifica dibujos competitivos; considera técnicas artísticas que ayudan a dirigir la búsqueda creativa de un estudiante en el camino del desarrollo artístico emocional.
