11 research outputs found
ΠΠ·Π°ΠΈΠΌΠΎΡΠ²ΡΠ·Ρ ΡΠΈΠΊΠ»Π° Π΄ΠΈΠΊΠ°ΡΠ±ΠΎΠ½ΠΎΠ²ΡΡ ΠΊΠΈΡΠ»ΠΎΡ Ρ ΡΠΈΠΊΠ»ΠΎΠΌ ΡΡΠΈΠΊΠ°ΡΠ±ΠΎΠ½ΠΎΠ²ΡΡ ΠΊΠΈΡΠ»ΠΎΡ Ρ Π²ΡΡΠΎΠΊΠΎΠΏΡΠΎΠ΄ΡΠΊΡΠΈΠ²Π½ΡΡ ΡΠ²ΠΈΠ½Π΅ΠΉ
The paper is the fundamental beginning of research series aimed at understanding the processes associated with high performance in higher animals. The research aim is to study correlation of dicarboxylic acid cycle with tricarboxylic acid cycle with establishment of activity and dislocation of enzymes, confirming the hypothesis of availability and active metabolic participation of peroxisome in highly productive animals. Research was conducted on the basis of the VNIIFBiP animal vivarium in 2019 with a group of piglets of the Irish Landrace breed (n = 10). After slaughter at the age of 210 days, the nuclear (with large tissue particles), mitochondrial and postmitochondrial fractions of the liver were studied with assessment of succinate dehydrogenase and activity of other dehydrogenes of the Krebs cycle. It was found that peroxisomes act as universal agents of communication and cooperation, and microtelets are able to generate various chemical signals that carry information, to control and arrange a number of mechanisms in the metabolic processes in the body. Despite the fact that the Krebs cycle dehydrogenases are considered mitochondrial enzymes, the experiment showed an increase in activity of priruvate dehydrogenase (P > 0.1), isocitrate dehydrogenase (0.1 > P > 0.05) and malate dehydrogenase (0.1 > P > 0.05), which, when comparing the mitochondrial and postmitochondrial fractions, indicates a higher activity of peroxisomal fractions. The peroxisome localization place is the postmitochondrial fraction, and the lower layer contains larger peroxisomes to a greater extent, while the upper layer contains smaller ones. It was found that indicator enzymes of glyoxylate cycle isocitratliase and malate synthase exhibit catalytic activity in the peroxisomal fraction of liver of highly productive pigs. The obtained data on functioning of key glyoxylate cycle enzymes and their intracellular compartmentalization in highly productive pigs allow learning more about the specifics of metabolism and its regulation processes. Application of this knowledge in practice opens up prospects for rationalizing the production of livestock products of increased quantity, improved quality with less feed, labor and financial resources spent.Π‘ΡΠ°ΡΡΡ ΡΠ²Π»ΡΠ΅ΡΡΡ ΡΡΠ½Π΄Π°ΠΌΠ΅Π½ΡΠ°Π»ΡΠ½ΡΠΌ Π½Π°ΡΠ°Π»ΠΎΠΌ ΡΠΈΠΊΠ»Π° ΡΠ°Π±ΠΎΡ, Π½Π°ΠΏΡΠ°Π²Π»Π΅Π½Π½ΡΡ
Π½Π° ΠΏΠΎΠ½ΠΈΠΌΠ°Π½ΠΈΠ΅ ΠΏΡΠΎΡΠ΅ΡΡΠΎΠ², ΡΠ²ΡΠ·Π°Π½Π½ΡΡ
Ρ Π²ΡΡΠΎΠΊΠΎΠΉ ΠΏΡΠΎΠ΄ΡΠΊΡΠΈΠ²Π½ΠΎΡΡΡΡ Ρ Π²ΡΡΡΠΈΡ
ΠΆΠΈΠ²ΠΎΡΠ½ΡΡ
. Π¦Π΅Π»Ρ ΡΠ°Π±ΠΎΡΡ β ΠΈΠ·ΡΡΠ΅Π½ΠΈΠ΅ Π²Π·Π°ΠΈΠΌΠΎΡΠ²ΡΠ·ΠΈ ΡΠΈΠΊΠ»Π° Π΄ΠΈΠΊΠ°ΡΠ±ΠΎΠ½ΠΎΠ²ΡΡ
ΠΊΠΈΡΠ»ΠΎΡ Ρ ΡΠΈΠΊΠ»ΠΎΠΌ ΡΡΠΈΠΊΠ°ΡΠ±ΠΎΠ½ΠΎΠ²ΡΡ
ΠΊΠΈΡΠ»ΠΎΡ Ρ ΡΡΡΠ°Π½ΠΎΠ²Π»Π΅Π½ΠΈΠ΅ΠΌ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΠΈ ΠΈ Π΄ΠΈΡΠ»ΠΎΠΊΠ°ΡΠΈΠΈ ΡΠ΅ΡΠΌΠ΅Π½ΡΠΎΠ², ΠΏΠΎΠ΄ΡΠ²Π΅ΡΠΆΠ΄Π΅Π½ΠΈΠ΅ Π³ΠΈΠΏΠΎΡΠ΅Π·Ρ ΠΎ Π½Π°Π»ΠΈΡΠΈΠΈ ΠΈ Π°ΠΊΡΠΈΠ²Π½ΠΎΠΌ ΠΌΠ΅ΡΠ°Π±ΠΎΠ»ΠΈΡΠ΅ΡΠΊΠΎΠΌ ΡΡΠ°ΡΡΠΈΠΈ ΠΏΠ΅ΡΠΎΠΊΡΠΈΡΠΎΠΌ Ρ Π²ΡΡΠΎΠΊΠΎΠΏΡΠΎΠ΄ΡΠΊΡΠΈΠ²Π½ΡΡ
ΠΆΠΈΠ²ΠΎΡΠ½ΡΡ
. ΠΡΡΠ»Π΅Π΄ΠΎΠ²Π°Π½ΠΈΡ ΠΏΡΠΎΠ²ΠΎΠ΄ΠΈΠ»ΠΈ Π½Π° Π±Π°Π·Π΅ Π²ΠΈΠ²Π°ΡΠΈΡ ΠΠΠΠΠ€ΠΠΈΠ ΠΆΠΈΠ²ΠΎΡΠ½ΡΡ
Π² 2019 Π³. Π½Π° Π³ΡΡΠΏΠΏΠ΅ ΠΏΠΎΡΠΎΡΡΡ ΠΏΠΎΡΠΎΠ΄Ρ ΠΈΡΠ»Π°Π½Π΄ΡΠΊΠΈΠΉ Π»Π°Π½Π΄ΡΠ°Ρ (n = 10). ΠΠΎΡΠ»Π΅ ΡΠ±ΠΎΡ Π² Π²ΠΎΠ·ΡΠ°ΡΡΠ΅ 210 Π΄Π½Π΅ΠΉ ΠΈΠ·ΡΡΠ΅Π½Ρ ΡΠ΄Π΅ΡΠ½Π°Ρ (Ρ ΠΊΡΡΠΏΠ½ΡΠΌΠΈ ΡΠ°ΡΡΠΈΡΠ°ΠΌΠΈ ΡΠΊΠ°Π½ΠΈ), ΠΌΠΈΡΠΎΡ
ΠΎΠ½Π΄ΡΠΈΠ°Π»ΡΠ½Π°Ρ ΠΈ ΠΏΠΎΡΡΠΌΠΈΡΠΎΡ
ΠΎΠ½Π΄ΡΠΈΠ°Π»ΡΠ½Π°Ρ ΡΡΠ°ΠΊΡΠΈΠΈ ΠΏΠ΅ΡΠ΅Π½ΠΈ Ρ ΠΎΡΠ΅Π½ΠΊΠΎΠΉ ΡΡΠΊΡΠΈΠ½Π°ΡΠ΄Π΅Π³ΠΈΠ΄ΡΠΎΠ³Π΅Π½Π°Π·Ρ ΠΈ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΠΈ Π΄ΡΡΠ³ΠΈΡ
Π΄Π΅Π³ΠΈΠ΄ΡΠΎΠ³Π΅Π½ΠΎΠ² ΡΠΈΠΊΠ»Π° ΠΡΠ΅Π±ΡΠ°. ΠΡΡΠ²Π»Π΅Π½ΠΎ, ΡΡΠΎ ΠΏΠ΅ΡΠΎΠΊΡΠΈΡΠΎΠΌΡ Π²ΡΡΡΡΠΏΠ°ΡΡ Π² ΠΊΠ°ΡΠ΅ΡΡΠ²Π΅ ΡΠ½ΠΈΠ²Π΅ΡΡΠ°Π»ΡΠ½ΡΡ
Π°Π³Π΅Π½ΡΠΎΠ² ΠΊΠΎΠΌΠΌΡΠ½ΠΈΠΊΠ°ΡΠΈΠΈ ΠΈ ΠΊΠΎΠΎΠΏΠ΅ΡΠ°ΡΠΈΠΈ, Π° ΠΌΠΈΠΊΡΠΎΡΠ΅Π»ΡΡΡ ΡΠΏΠΎΡΠΎΠ±Π½Ρ Π³Π΅Π½Π΅ΡΠΈΡΠΎΠ²Π°ΡΡ ΡΠ°Π·Π»ΠΈΡΠ½ΡΠ΅ Ρ
ΠΈΠΌΠΈΡΠ΅ΡΠΊΠΈΠ΅ ΡΠΈΠ³Π½Π°Π»Ρ, ΠΏΠ΅ΡΠ΅Π½ΠΎΡΡΡΠΈΠ΅ ΠΈΠ½ΡΠΎΡΠΌΠ°ΡΠΈΡ, ΠΏΠΎ ΠΊΠΎΠ½ΡΡΠΎΠ»Ρ ΠΈ ΡΠΏΡΠ°Π²Π»Π΅Π½ΠΈΡ ΡΡΠ΄ΠΎΠΌ ΠΌΠ΅Ρ
Π°Π½ΠΈΠ·ΠΌΠΎΠ² Π² ΠΌΠ΅ΡΠ°Π±ΠΎΠ»ΠΈΡΠ΅ΡΠΊΠΈΡ
Π²Π·Π°ΠΈΠΌΠΎΠΎΡΠ½ΠΎΡΠ΅Π½ΠΈΡΡ
ΠΎΡΠ³Π°Π½ΠΈΠ·ΠΌΠ°. ΠΠ΅ΡΠΌΠΎΡΡΡ Π½Π° ΡΠΎ ΡΡΠΎ Π΄Π΅Π³ΠΈΠ΄ΡΠΎΠ³Π΅Π½Π°Π·Ρ ΡΠΈΠΊΠ»Π° ΠΡΠ΅Π±ΡΠ° ΡΡΠΈΡΠ°ΡΡΡΡ ΠΌΠΈΡΠΎΡ
ΠΎΠ½Π΄ΡΠΈΠ°Π»ΡΠ½ΡΠΌΠΈ ΡΠ΅ΡΠΌΠ΅Π½ΡΠ°ΠΌΠΈ, Π² ΡΠΊΡΠΏΠ΅ΡΠΈΠΌΠ΅Π½ΡΠ΅ Π½Π°Π±Π»ΡΠ΄Π°Π»ΠΎΡΡ ΡΠ²Π΅Π»ΠΈΡΠ΅Π½ΠΈΠ΅ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΠΈ ΠΏΡΠΈΡΡΠ²Π°ΡΠ΄Π΅Π³ΠΈΠ΄ΡΠΎΠ³Π΅Π½Π°Π·Ρ (Π > 0,1), ΠΈΠ·ΠΎΡΠΈΡΡΠ°ΡΠ΄Π΅Π³ΠΈΠ΄ΡΠΎΠ³Π΅Π½Π°Π·Ρ (0,1 > Π > 0,05) ΠΈ ΠΌΠ°Π»Π°ΡΠ΄Π΅Π³ΠΈΠ΄ΡΠΎΠ³Π΅Π½Π°Π·Ρ (0,1 > Π > 0,05), ΡΡΠΎ ΠΏΡΠΈ ΡΡΠ°Π²Π½Π΅Π½ΠΈΠΈ ΠΌΠ΅ΠΆΠ΄Ρ ΡΠΎΠ±ΠΎΠΉ ΠΌΠΈΡΠΎΡ
ΠΎΠ½Π΄ΡΠΈΠ°Π»ΡΠ½ΠΎΠΉ ΠΈ ΠΏΠΎΡΡΠΌΠΈΡΠΎΡ
ΠΎΠ½Π΄ΡΠΈΠ°Π»ΡΠ½ΠΎΠΉ ΡΡΠ°ΠΊΡΠΈΠΉ ΡΠΊΠ°Π·ΡΠ²Π°Π΅Ρ Π½Π° ΠΏΡΠΎΡΠ²Π»Π΅Π½ΠΈΠ΅ Π±ΠΎΠ»Π΅Π΅ Π²ΡΡΠΎΠΊΠΎΠΉ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΠΈ ΠΏΠ΅ΡΠΎΠΊΡΠΈΡΠΎΠΌΠ°Π»ΡΠ½ΡΡ
ΡΡΠ°ΠΊΡΠΈΠΉ. ΠΠ΅ΡΡΠΎ Π»ΠΎΠΊΠ°Π»ΠΈΠ·Π°ΡΠΈΠΈ ΠΏΠ΅ΡΠΎΠΊΡΠΈΡΠΎΠΌ β ΠΏΠΎΡΡΠΌΠΈΡΠΎΡ
ΠΎΠ½Π΄ΡΠΈΠ°Π»ΡΠ½Π°Ρ ΡΡΠ°ΠΊΡΠΈΡ, Π² Π½ΠΈΠΆΠ½Π΅ΠΌ ΡΠ»ΠΎΠ΅ ΡΠΎΡΡΠ΅Π΄ΠΎΡΠΎΡΠ΅Π½Ρ Π² Π±ΠΎΠ»ΡΡΠ΅ΠΉ ΡΡΠ΅ΠΏΠ΅Π½ΠΈ ΠΊΡΡΠΏΠ½ΡΠ΅ ΠΏΠ΅ΡΠΎΠΊΡΠΈΡΠΎΠΌΡ, Π° Π² Π²Π΅ΡΡ
Π½Π΅ΠΌ ΡΠ»ΠΎΠ΅ β Π±ΠΎΠ»Π΅Π΅ ΠΌΠ΅Π»ΠΊΠΈΠ΅. Π£ΡΡΠ°Π½ΠΎΠ²Π»Π΅Π½ΠΎ, ΡΡΠΎ ΠΈΠ½Π΄ΠΈΠΊΠ°ΡΠΎΡΠ½ΡΠ΅ ΡΠ΅ΡΠΌΠ΅Π½ΡΡ Π³Π»ΠΈΠΎΠΊΡΠΈΠ»Π°ΡΠ½ΠΎΠ³ΠΎ ΡΠΈΠΊΠ»Π° ΠΈΠ·ΠΎΡΠΈΡΡΠ°ΡΠ»ΠΈΠ°Π·Π° ΠΈ ΠΌΠ°Π»Π°ΡΡΠΈΠ½ΡΠ°Π·Π° ΠΏΡΠΎΡΠ²Π»ΡΡΡ ΠΊΠ°ΡΠ°Π»ΠΈΡΠΈΡΠ΅ΡΠΊΡΡ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΡ Π² ΠΏΠ΅ΡΠΎΠΊΡΠΈΡΠΎΠΌΠ°Π»ΡΠ½ΠΎΠΉ ΡΡΠ°ΠΊΡΠΈΠΈ ΠΏΠ΅ΡΠ΅Π½ΠΈ Π²ΡΡΠΎΠΊΠΎΠΏΡΠΎΠ΄ΡΠΊΡΠΈΠ²Π½ΡΡ
ΡΠ²ΠΈΠ½Π΅ΠΉ. ΠΠΎΠ»ΡΡΠ΅Π½Π½ΡΠ΅ Π΄Π°Π½Π½ΡΠ΅ ΠΎ ΡΡΠ½ΠΊΡΠΈΠΎΠ½ΠΈΡΠΎΠ²Π°Π½ΠΈΠΈ Ρ Π²ΡΡΠΎΠΊΠΎΠΏΡΠΎΠ΄ΡΠΊΡΠΈΠ²Π½ΡΡ
ΡΠ²ΠΈΠ½Π΅ΠΉ ΠΊΠ»ΡΡΠ΅Π²ΡΡ
ΡΠ΅ΡΠΌΠ΅Π½ΡΠΎΠ² Π³Π»ΠΈΠΎΠΊΡΠΈΠ»Π°ΡΠ½ΠΎΠ³ΠΎ ΡΠΈΠΊΠ»Π° ΠΈ ΠΈΡ
Π²Π½ΡΡΡΠΈΠΊΠ»Π΅ΡΠΎΡΠ½ΠΎΠΉ ΠΊΠΎΠΌΠΏΠ°ΡΡΠΌΠ΅Π½ΡΠ°Π»ΠΈΠ·Π°ΡΠΈΠΈ ΠΏΠΎΠ·Π²ΠΎΠ»ΡΡΡ Π³Π»ΡΠ±ΠΆΠ΅ ΠΏΠΎΠ·Π½Π°ΡΡ ΡΠΏΠ΅ΡΠΈΡΠΈΠΊΡ ΠΎΠ±ΠΌΠ΅Π½Π° Π²Π΅ΡΠ΅ΡΡΠ² ΠΈ ΠΏΡΠΎΡΠ΅ΡΡΠΎΠ² Π΅Π³ΠΎ ΡΠ΅Π³ΡΠ»ΡΡΠΈΠΈ. ΠΡΠΈΠΌΠ΅Π½Π΅Π½ΠΈΠ΅ ΡΡΠΈΡ
Π·Π½Π°Π½ΠΈΠΉ Π½Π° ΠΏΡΠ°ΠΊΡΠΈΠΊΠ΅ ΠΎΡΠΊΡΡΠ²Π°Π΅Ρ ΠΏΠ΅ΡΡΠΏΠ΅ΠΊΡΠΈΠ²Ρ ΡΠ°ΡΠΈΠΎΠ½Π°Π»ΠΈΠ·Π°ΡΠΈΠΈ ΠΏΡΠΎΠΈΠ·Π²ΠΎΠ΄ΡΡΠ²Π° ΠΆΠΈΠ²ΠΎΡΠ½ΠΎΠ²ΠΎΠ΄ΡΠ΅ΡΠΊΠΎΠΉ ΠΏΡΠΎΠ΄ΡΠΊΡΠΈΠΈ ΠΏΠΎΠ²ΡΡΠ΅Π½Π½ΠΎΠ³ΠΎ ΠΊΠΎΠ»ΠΈΡΠ΅ΡΡΠ²Π°, ΡΠ»ΡΡΡΠ΅Π½Π½ΠΎΠ³ΠΎ ΠΊΠ°ΡΠ΅ΡΡΠ²Π° Ρ ΠΌΠ΅Π½ΡΡΠΈΠΌΠΈ Π·Π°ΡΡΠ°ΡΠ°ΠΌΠΈ ΠΊΠΎΡΠΌΠΎΠ², ΡΡΡΠ΄Π° ΠΈ ΡΠΈΠ½Π°Π½ΡΠΎΠ²ΡΡ
ΡΡΠ΅Π΄ΡΡΠ² Π½Π° Π΅Π΅ ΠΏΡΠΎΠΈΠ·Π²ΠΎΠ΄ΡΡΠ²ΠΎ
Innovative development scenario of the domestic market ofΒ meat products: problems, factors, trends
The market for meat and its products is, on the one hand, one of the criteria for a country's food security, and, on the other, a peculiar social indicator, since it is a supplier of animal protein that plays an important role in ensuring healthy nutrition of the human body, which directly affects the quality of life., human development index, the formation and creation of conditions for its reproduction. The aim of the work is to study the domestic market of meat processing products from the standpoint of the implementation of the innovative scenario of its development, taking into account the orientation on mental changes in the consumer audience, the tendency to change the hedonic preferences of end users of meat products in the light of the evolution of nutrition theories. The subject of the study was trends, problems and prospects for the development of the domestic market of meat products, including taking into account the peculiarities of the consumer mentality, psychological perception of meat products in the light of the development of the theory and practice of healthy eating. The research methodology was based on a complex of general scientific methods, including analytical, synthetic, deduction. The basis of the research was the compilation and analysis of information sources in the subject area of ??the state and development prospects of the global and domestic meat and meat products market, which form plausible development scenarios, from the standpoint of analyzing commercial relations inherent in the b2c (busness-to-consumer) sector, in particular, the role assortment and the role of the individual customer. The characteristics, factors and trends of the innovation scenario of the development of the market of chilled and frozen meat products are formulated. The perspectives of combining the concept of healthy nutrition with the idea of reviving the traditions of national cuisine based on convergence with innovative food biotechnologies, including based on the author's innovative project to develop combined food systems and economically efficient meat products
Marketing potential of combined meat-plant food products as innovative consumer objects
For the growth of the consumer potential of the food market, an active search for innovative ways and means of development, taking into account various sources of innovative opportunities, is necessary. The analysis shows that consumers of products of agro-industrial enterprises, catering and trade enterprises are an important, but insufficiently studied element in the system of generating samples, or ideas, innovative consumer objects. The purpose of the work is to study consumer trends, features of segmentation in the customer typology and customer feedback elements, as sources of innovation in the external environment of various enterprises and organizations for the production of food based on the processing of meat raw materials. The object of the research was the regional market of meat products of the Central Black Soil Region on the example of the city of Voronezh and the city of Liski, Voronezh Region. The subject of research was the direction of improving the range of meat and meat-plant products, corresponding to the innovative scenario of the development of their market. The analysis of consumer preferences and motivations of the population of the Central Black Earth region (for example, the city of Voronezh and the city of Liski, Voronezh region) in relation to the combined meat and vegetable products was carried out and their potential as innovative consumer objects was evaluated. The article implements a questionnaire survey method in relation to the psychological perception of protein foods from consumers, including middle and mature age. The survey revealed data on the popularity of types of meat products, the frequency of their consumption, priority properties for the consumer, storage modes. The expediency of increasing the nutritional and biological value and the formation of consumer properties of combined meat products based on the hedonic preferences of consumer groups has been substantiated. Directions for improving the range of products for processing meat raw materials will be an organic addition to the cluster for the production and processing of specialized breeds of beef cattle, pork, and poultry meat in the Voronezh region and the Central Black Earth region as a whole
PROTECTIVE ACTIVITY OF NOVEL BENZIMIDAZOLE DERIVATIVES AT EXPERIMENTAL INFLUENZA INFECTION
Influenza is an acute respiratory viral infection, which represents an important health problem. Every year, influenzaΒ causes epidemicsΒ and pandemics, leading to increase in morbidity and mortality in allΒ regions of the globe. Due to the segmentalΒ organization of theΒ genome and low accuracy of its replication, the influenza virus isΒ capable of escaping the hostβs immuneΒ response (antigenic drift), asΒ well as the selection of drug-resistant variants. This calls forΒ constant monitoring of the sensitivityΒ of viral isolates to antiviralΒ drugs and the development of new etiotropic antiviral agents thatΒ have alternative targets andΒ mechanisms of activity. The purpose ofΒ this study was to characterize the new aminobenzimidazoleΒ derivatives as protectiveΒ agents in lethal influenza infection in whiteΒ mice. The efficacy of the compounds was assessed by their ability toΒ reduce specificΒ mortality of animals in the course of lethal influenzaΒ pneumonia caused by the influenza A/Puerto Rico/8/34 (H1N1)Β irus,Β increase the life duration of animals, and normalize theΒ morphological structure of lung tissue comparing to the placeboΒ group.Β For all the compounds studied, a decrease in the specificΒ mortality of animals (from 20 to 60%) has been shown. TheΒ referenceΒ drug (oseltamivir phosphate) reduced the mortality ofΒ mice by 80%. The benzimidazole derivative 2519 demonstratedΒ theΒ highest indices of protective activity, its use reduced the mortality ofΒ animals by 60% and increased their mean day of deathΒ by 1.6 days in comparison with the control group. Morphological analysis showed that the activity of derivative 2519 was manifestedΒ in theΒ normalization of the morphological structure of lung tissue in theΒ course of influenza pneumonia. On day 5 afterΒ infection, the cells ofΒ the bronchial epithelium looked intact, in contrast to destroyed cellsΒ with numerous viral inclusionsΒ in control animals. The foci ofΒ inflammation themselves occupied a smaller area compared to theΒ control. At the same time,Β there was no correlation between theΒ previously obtained data on the virus-inhibiting effect of theseΒ compounds in vitro andΒ the data obtained in animals. This suggestsΒ that despite the presence of direct antiviral activity detectedΒ previously in in vitroΒ experiments, the protective properties of theΒ studied aminobenzimidazoles on animals are caused, in addition toΒ the etiotropicΒ effect, by other pathogenetic factors. In conclusion,Β amino derivatives of benzimidazole should be considered asΒ compoundsΒ that are promising for further development andΒ introduction as an anti-influenza agents
Synthesis and antimicrobial activity of adamantyl substituted pyridoxine derivatives
Β© 2019 Bentham Science Publishers Background: Adamantane derivatives possess multiple pharmacological activities such as antiviral, anticancer, antimycobacterial, antidiabetic, antiparkinsonian and others. The interest of medicinal chemists in adamantane compounds is due to their unique spatial structure, high lipophilicity, and carbon cage rigidity. As a result, these molecules can easily penetrate biological lipid membranes and often have unique target-specific activity profile. Another pharmacophore studied in this work is pyridoxine (vitamin B6). Pyridoxine plays highly important roles in living cells as a key cofactor of many enzymes. On the other hand, its molecular scaffold is a valuable structural platform which has led to the development of several launched drugs (Pyritinol, Pirisudanol, Cycletanine, Mangafodipir) and a wide number of preclinical and clinical drug candidates. Objective: The objective of this study is a synthesis of pyridoxine-adamantane and pyridoxinecyclooctane dipharmacophore molecules. The underlying idea was to assess the antibacterial and antiviral potential of such dipharmacophores, based on multiple examples of promising antiinfective agents which have in their structures adamantane and pyridoxine moieties. Another specific reason was to explore the ability of pyridoxine pharmacophore to suppress the potential of microbial pathogens to develop resistance to drug molecules. Methods: In this study, a series of pyridoxine-adamantane and pyridoxine-cyclooctane dipharmacophore molecules were synthesized based on reactions of three different cycloalkyl amines with the corresponding electrophilic derivatives of pyridoxine aldehydes, chlorides and acetates. All synthesized compounds have been tested for their in vitro activity against M. tuberculosis H37Rv strain and H3N2 (A/Aichi/2/68) influenza virus. Results: Series of pyridoxine-adamantane and pyridoxine-cyclooctane dipharmacophore molecules were synthesized based on reactions of three different cycloalkylamines with the corresponding electrophilic derivatives of pyridoxine aldehydes, chlorides and acetates. Reaction of cycloalkylamines with pyridoxine derivatives, in which meta-hydroxyl and ortho-hydroxymethyl groups are protected by acetyl groups, represents a useful alternative to reductive amination of aldehydes and nucleophilic substitution of alkyl halides. According to a tentative mechanism, it proceeds via paraand ortho-pyridinone methides which readily react with nucleophiles. None of the synthesized dipharmacophore compounds showed activity against M. tuberculosis H37Rv strain. At the same time, three compounds demonstrated some antiviral activity against H3N2 (A/Aichi/2/68) influenza virus (EC50 52-88 ΞΌg/mL) that was comparable to the activity of Amantadine, though lower than the activity of Rimantadine. The results of this work can be useful in the design of physiologically active derivatives of pyridoxine and adamantane. Conclusion: The results of this work can be useful in the design of physiologically active derivatives of pyridoxine and adamantane