Current issues in pharmacy and medicine: science and practice最新文献

{"title":"Conceptual and terminological apparatus for disciplinary responsibility in pharmaceutical activity","authors":"O. H. Aleksieiev","doi":"10.14739/2409-2932.2023.2.277085","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.2.277085","url":null,"abstract":"The analysis of the content of the norm and its interpretation by the Constitutional Court of Ukraine leads to the conclusion that the labor legislation does not comply with the requirements of the Constitution of Ukraine, and the emphasis is placed on the need to harmonize the relevant norms with the Basic Law.\u0000The aim of the work is to analyze the modern problem of terminological aspects of disciplinary responsibility in pharmaceutical activity according to the current legislation.\u0000Materials and methods. The research was conducted using comparative legal, historical methods, methods of analysis and synthesis.\u0000Results. Attention is paid to the problems of legislation related to the lack of a special approach to the regulation of disciplinary responsibility in pharmaceutical activity. It is noted that at the moment, a regime of general disciplinary responsibility has been established for pharmaceutical workers. Citing examples of the regulation of disciplinary responsibility in the pharmaceutical activity of developed countries, it is indicated that the modern national legislative approach does not correspond to the international practice of building a public health care system.\u0000Conclusions. The establishment of a regime of special disciplinary responsibility for pharmaceutical workers is substantiated, which should include the creation of a special body that will be empowered to consider disciplinary proceedings and make a decision on the imposition of disciplinary sanctions, a special procedure for considering disciplinary proceedings, an expanded list of types of disciplinary sanctions.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"43 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85823353","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The justification of the optimal composition and research of a local hemostatic agent based on naturally occurring polysaccharides","authors":"V. V. Hladyshev, S. Sоkolovskyi, I. Sobko, Uģis Klētnieks, Audrius Butkevichius","doi":"10.14739/2409-2932.2023.2.281238","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.2.281238","url":null,"abstract":"The analysis of existing methods and products for controlling bleeding reveals that medical means exhibit significantly higher efficacy compared to mechanical methods of achieving hemostasis. However, it is important to note that medical means cannot entirely replace surgical hemostasis in cases of severe bleeding from large veins and arteries. In emergency situations, such as during military conflicts or workplace injuries, the use of local contact hemostatic agents is preferred. These agents do not require specialized skills for application, making them accessible to individuals in need of immediate assistance. If included in a first-aid kit, these agents enable victims to address minor injuries promptly and control bleeding. In critical bleeding situations, any nearby individual can use the tool to provide aid. Given the ongoing military activities within our country’s territory, the development of effective domestic hemostatic agents has become an urgent priority. This initiative aims to ensure the availability of such products to our military personnel.\u0000Aim. The aim of this work is to justify the optimal composition of a local hemostatic agent based on readily available raw materials and feasible technologies.\u0000Materials and methods. After conducting an extensive review of domestic and foreign literature, the basis for the development of the future contact hemostatic agent was chosen to be adsorbing materials derived from biologically active components of mineral, synthetic, phyto-, and organic origins.\u0000The focus of this study is on natural polysaccharides with potential hemostatic activity, specifically alginate, kappa carrageenan, guar gum, and xanthan gum. One key property of polysaccharides is their ability to swell, which positively influences hemostasis. The hemostatic effect of model hemostatic compositions was evaluated using a femoral artery bleeding model induced by mechanical damage. Additionally, a model involving capillary-parenchymal bleeding from a laceration wound on the liver in adult rats was employed for further investigation.\u0000Results. Experimental studies have provided evidence of the hemostatic effect of natural polysaccharides due to their water absorption and swelling properties. In comparison with well-known medical products Celox and Revul®, substances with hemostatic activity, including alginate, kappa carrageenan GU 805, and the comparative drug Celox, have demonstrated significant reductions in bleeding time. Specifically, alginate, kappa carrageenan GU 805, and Celox have shown reductions of 38 %, 53 %, and 57 % respectively, compared to the positive control (PC) group. To enhance the hemostatic activity, a combination of the leading compounds with the addition of 7 % calcium gluconate was developed. The inclusion of calcium gluconate in the combination is associated with the involvement of calcium ions in all stages of blood coagulation, thereby increasing the overall hemostatic effect of the combination.\u0000Based o","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"63 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80321417","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis, molecular docking, and ADME analysis of a series of 4-amino-3,5-dimethyl-1,2,4-triazole derivatives","authors":"L. I. Kucherenko, T. Brytanova, A. S. Hotsulia","doi":"10.14739/2409-2932.2023.2.281039","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.2.281039","url":null,"abstract":"The heterocyclic system of 1,2,4-triazole enables the successful creation of promising biologically active compounds. By creating a range of derivatives based on 4-amino-3,5-dimethyl-1,2,4-triazole, the spectrum of potential biologically active compounds can be expanded.\u0000The aim of the work was the synthesis and in silico justification of the prospects for the search for biologically active compounds among 4-amino-3,5-dimethyl-1,2,4-triazole derivatives.\u0000Materials and methods. The work uses modern methods for synthesizing organic compounds, followed by confirmation of their individuality and structure through the analysis of physical-chemical parameters and spectroscopic techniques such as 1H NMR, IR spectroscopy, elemental analysis, and chromatography-mass spectrometry. To assess the similarity of the synthesized compounds to medicinal products, the SwissADME online tool was employed. The probability of impact on a number of enzyme systems (cyclooxygenase-2, lanosterol 14α-demethylase, anaplastic lymphoma kinase) was estimated using molecular docking.\u0000Results. A series of newly synthesized derivatives of 4-amino-3,5-dimethyl-1,2,4-triazole was obtained, and the synthesis conditions were optimized and their structures were confirmed. It was determined that there is a high probability of influencing lanosterol 14α-demethylase, highlighting the significance of further research on the antifungal activity of the synthesized compounds. Additionally, the potential influence on the activity of cyclooxygenase-2 and anaplastic lymphoma kinase was discovered. However, the probability of exhibiting the corresponding activities, namely anti-inflammatory and anti-cancer, is low. Physical indicators, parameters of pharmacokinetics, and drug-likeness are important, which determines the prospects of creating biologically active substances based on the synthesized series of compounds.\u0000Conclusions. A series of 4-((R-iden)amino)-3,5-dimethyl-1,2,4-triazoles were synthesized, and their general physical-chemical properties were determined. The overall potential for creating innovative biological products based on these compounds was assessed using in silico methods for predicting the activity of substances.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"18 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86908993","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of a method for the quantitative determination of glibenclamide in tablets","authors":"L. H. Leleka, S. O. Vasuik","doi":"10.14739/2409-2932.2023.2.274336","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.2.274336","url":null,"abstract":"Aim. To develop and validate a spectrophotometric technique for quantitative determination of glibenclamide in tablets by reaction with 2,3-dichloro-1,4-naphthoquinone.\u0000Materials and methods. In the study, the substance glibenclamide of pharmacopoeial purity was used, tablets – “Maninil” 5 mg and “Glibenclamid-Zdorovye” 5 mg, 2,3-dichloro-1,4-naphthoquinone of the “CFA” qualification was chosen as a reagent, as a solvent – dimethylformamide (DMF) “CFA”.\u0000The following analytical equipment was used for the research: spectrophotometer “Specord-200” (Analytic Jena AG, Germany), water bath “MEMMERT WNB7”, laboratory electronic scales RADWAG XA 210. 4Y, measuring laboratory vessels of class A.\u0000Results. A new, simple spectrophotometric method of quantitative determination of glibenclamide in tablets by reaction with 2,3-dichloro-1,4-naphthoquinone in DMF medium was developed. The absorption maximum was at 489–491 nm. The value of the detection limit is 10.9 μg/ml, which indicates sufficient sensitivity of the reaction.\u0000Subordination to the basic law of light absorption is within the limits of concentrations of 13.7–27.4 mg/100 ml. In the process of developing the methodology, the following validation characteristics were determined: specificity, linearity, precision, correctness, and robustness.\u0000Conclusions. The methodology for the quantitative determination of glibenclamide was developed and validated according to the requirements of the State Pharmacopoeia of Ukraine. It has been proven that the method is simple, accessible, and validated for such characteristics as linearity, convergence and robustness and can be used for application in laboratories for quality control of medicinal products.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"5 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78675892","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A clinical case of diagnosis of autoimmune hepatitis at the stage of liver cirrhosis","authors":"O. Svitlytska, O. Riabokon, A. O. Svitlytskyі, N. H. Horbatkova, E. V. Kotliarevska","doi":"10.14739/2409-2932.2023.2.277495","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.2.277495","url":null,"abstract":"The aim of the work is to analyze a clinical case of autoimmune hepatitis (АІН) diagnosis at the stage of cirrhosis in a 40-year-old female patient and to remind practicing doctors about the serious consequences of this disease.\u0000Materials and methods. A clinical case of AIH diagnosed according to the criteria of the International Autoimmune Hepatitis Group (2008) at the stage of cirrhosis in a 40-year-old female patient was analyzed. A puncture liver biopsy with a morphological study of the hepatobioptate was also performed to verify the diagnosis.\u0000Results. The analysis of the clinical case of AIH in a 40-year-old female patient revealed a delayed diagnosis of AIH at the cirrhosis stage. This was due to the absence of any clinical symptoms of the disease for a long period of time, and the lack of attention of practicing doctors in investigating the reasons for the long-term increase in transaminase activity. The trigger factor for the clinical manifestations of cirrhosis, which developed due to the long-term course of AIH, was emotional stress resulting from leaving the combat zone.\u0000The application of the International Autoimmune Hepatitis Group criteria in clinical practice was demonstrated, specifically the combination of elevated antinuclear antibodies and total IgG, characteristic histological changes in the liver, and exclusion of hepatotropic viral infections, which allowed for a reliable diagnosis of AIH.\u0000Medical treatment resulted in certain positive changes in clinical and laboratory indicators. However, according to the transplant doctor’s opinion, at this stage of the AIH course, the patient required a liver transplant and therefore was added to the waiting list.\u0000Conclusions. This clinical case highlights the late diagnosis of AIH at the cirrhosis stage in a 40-year-old female patient due to the absence of clinical manifestations over several years and the lack of vigilance among doctors, possibly primary care physicians or specialists, to investigate the persistent increase in transaminase activity. The application of the International Autoimmune Hepatitis Group criteria helped confirm the diagnosis of AIH.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73224414","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and properties of 6-(2,6-dichlorophenyl)-3- (3-methyl-1H-pyrazol-5-yl)-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b] [1,3,4]thiadiazine-7-carboxylic acid and its salts","authors":"S. Fedotov, A. S. Hotsulia","doi":"10.14739/2409-2932.2023.2.279460","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.2.279460","url":null,"abstract":"Carboxylic acids and their derivatives are an important component of many biological processes. For example, they can be used to create new medicines that can be useful in the fight against various diseases. Additionally, compounds containing a thiazole moiety may possess beneficial properties in practical pharmacy. The incorporation of this heterocyclic structure in molecules can positively impact several biological characteristics, such as anti-inflammatory, antiviral, and antifungal activities.\u0000Consequently, exploring novel compounds that combine a thiazole fragment with a carboxyl group holds promise for the advancement of new drugs and diagnostic tools that can contribute significantly to the battle against numerous diseases.\u0000The aim of the work was to create a number of organic and inorganic salts of 6-(2,6-dichlorophenyl)-3-(3-methyl-1H-pyrazol-5-yl)-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-7-carboxylic acid and study of their properties, as well as selective determination of the biological potential of these compounds.\u0000Materials and methods. The synthetic part of the study involved the sequential synthesis of the original compound 4-amino-5-(3-methyl-1H-pyrazol-5-yl)-1,2,4-triazole-3-thiol using a well-established method described in previous articles. The next stage involved the reaction of thiol with 2,3-dichlorobenzaldehyde in a medium of glacial acetic acid. The resulting Schiff base was subsequently reacted with 2-chloroethanoic acid in tetrahydrofuran in the presence of an equimolar amount of sodium hydride.\u0000Salts of the corresponding acid were formed during the reaction of 6-(2,6-dichlorophenyl)-3-(3-methyl-1H-pyrazol-5-yl)-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-7-carboxylic acid with both organic and inorganic bases in an aqueous-alcohol medium. The structures of all synthesized compounds were determined using 1H NMR spectroscopy and elemental analysis. Additionally, the individuality of each compound was confirmed using high-performance liquid chromatography-mass spectrometry.\u0000Results. The study determined the optimal conditions for the formation of both organic and inorganic salts of 6-(2,6-dichlorophenyl)-3-(3-methyl-1H-pyrazol-5-yl)-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-7-carboxylic acid. The analysis of pharmacokinetic parameters and physicochemical properties using ADME (absorption, distribution, metabolism, and excretion) allowed for the identification of promising synthesized compounds and the selection of more optimal compounds for further investigation.\u0000Conclusions. The structure of 12 compounds was synthesized and confirmed. Physical-chemical and pharmacokinetic analysis of ADME parameters was carried out and promising compounds were selected for more in-depth research.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88928159","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Complex applying physical therapy and preformed physical factors in pregnant women with chronic pyelonephritis","authors":"М. І. Pavliuchenko, V. H. Siusiuka, N. V. Haidai, M. Serhiienko, O. Deinichenko","doi":"10.14739/2409-2932.2023.1.269150","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.1.269150","url":null,"abstract":"The aim of the work is to evaluate the impact of physical therapy and preformed physical factors in pregnant women with chronic pyelonephritis on central hemodynamic indicators.\u0000Materials and methods. The dynamics of 134 pregnant women with chronic pyelonephritis (CP) in the remission stage, who underwent a complex sanatorium rehabilitation program, were examined. The main study group consisted of 79 pregnant women with chronic pyelonephritis. In this contingent of women, the sanatorium rehabilitation complex additionally included a course of intermittent normobaric hypoxytherapy (INH). The comparison group consisted of 55 pregnant women with CP, for whom the sanatorium rehabilitation complex did not include an INH course. The control group is represented by 37 somatically healthy women with a physiological course of pregnancy. All pregnant women were examined for central hemodynamic (CH) indicators using the computer diagnostic complex REOKOM (Kharkiv).\u0000Results. Pregnancy periods of 20–30 and 31–30 weeks in women with CP are characterized by a pathological load on central hemodynamics. At the same time, the application for the INH course in the sanatorium rehabilitation complex (the main group) allows for an increase in the compensatory capabilities of the pregnant woman with CH. Thus, in the period of pregnancy of 22–30 weeks in the main group, indicators of diastolic blood pressure and heart rate were probably lower than the control values (P < 0.001), which in this group is determined by values of peripheral resistance of blood vessels close to those of the control group (P > 0.05), regardless of the timing of the study.\u0000The study of CH and the comparison of different periods of gestation and between research groups indicate an inverse relationship between indicators that reflect the intensity of cardiohemodynamics and indicators of vascular resistance, as one of the final mechanisms of maintaining blood pressure at a physiological level, or its pathological increase in chronic pyelonephritis and preeclampsia\u0000Taking into account that the ratio of cardiac index indicators and total peripheral vascular resistance in all study groups was stable and directly dependent on the level of blood pressure, it is advisable to recommend for practical application in order to assess the state of CH of pregnant women with CP indicators of stroke or cardiac indices, which characterize the intensity cardiohemodynamics and do not depend on the anthropometric data of the pregnant woman.\u0000Conclusions. The application of physical therapy and preformed physical factors, namely, intermittent normobaric hypoxytherapy in pregnant women with chronic pyelonephritis in a complex program of sanatorium rehabilitation increases the compensatory capabilities of the cardiovascular system, which is confirmed by a significant decrease in the values of the total peripheral resistance against the background of an increase in the cardiac index.\u0000 ","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"50 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81785576","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and properties of S-alkyl 4-amino-5-(5-(3-fluorophenyl)-pyrazol-3-yl)-1,2,4-triazole-3-thiol derivatives","authors":"S. Fedotov, C. A. S. Hotsulia A, С. О. Федотов, А. С. Гоцуля","doi":"10.14739/2409-2932.2023.1.273461","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.1.273461","url":null,"abstract":"An important direction of modern pharmaceutical science is the creation of promising biologically active compounds, which in the hands of scientists can be transformed into effective medicinal products. Heterocyclic compounds are the undisputed leader in solving this problem. A well-known fact and a well-founded approach to achieving the desired pharmacological effect is the combination of different heterocyclic fragments in the structure of one molecule. And here it makes sense to focus our attention on such heterocycles as pyrazole and 1,2,4-triazole. After all, a number of well-known medicines have already been invented on their basis. Thus, the construction of a chemical tandem with heterocyclic blocks of the specified nature is an actual and promising direction of scientific work.\u0000The aim of the work was to create a number of S-alkyl derivatives of 4-amino-5-(5-(3-fluorophenyl)pyrazol-3-yl)-1,2,4-triazole-3-thiol and study their properties, as well as preliminary selective establishment biological potential of these compounds.\u0000Materials and methods. The synthesis of the target products of chemical transformation was successfully implemented by the step-by-step use of well-known methods of organic synthesis. Thus, the first stage was successfully implemented with the help of available reagents, the role of which was performed by diethyl oxalate and 1-(3-fluorophenyl)ethan-1-one with the participation of sodium methylate. The next stage involved hydrazinolysis. Subsequently, the corresponding potassium xanthogenate was successfully synthesized, which was subsequently transformed under the action of hydrazine hydrate into the target 4-amino-5-(5-(3-fluorophenyl)pyrazol-3-yl)-1,2,4-triazole-3-thiol. The next stage was S-alkylation. The structure of all synthesized substances was determined with IR spectrophotometry, 1H NMR spectroscopy, and elemental analysis. The individuality of the compounds was confirmed by high-performance liquid chromatography-mass spectrometry. In silico studies were carried out with well-known software products, namely: AutoDock Vina, Biovia Discovery Studio, Hyper Chem 7.5, and Open Babel. Cyclooxygenase-2, lanosterol 14α-demethylase, and anaplastic lymphoma kinase were used as model enzymes.\u0000Results. The optimal conditions for the stepwise creation of S-alkyl derivatives of 4-amino-5-(5-(3-fluorophenyl)pyrazol-3-yl)-1,2,4-triazole-3-thiol were established and the preparation of the specified compounds was carried out. The use of molecular docking made it possible to determine the perspective of further research on anti-inflammatory, antifungal, and antitumor properties in a number of synthesized structures.\u0000Conclusions. S-alkyl derivatives of 4-amino-5-(5-(3-fluorophenyl)pyrazol-3-yl)-1,2,4-triazole-3-thiol are reasonably promising objects for the study of antifungal activity.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83933330","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ozonolytic synthesis of 2-hydroxybenzyl alcohol for the production of gastrodin","authors":"A. Halstian, A. Hasanova, H. Tarasenko","doi":"10.14739/2409-2932.2023.1.272608","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.1.272608","url":null,"abstract":"2-Hydroxybenzyl alcohol is an important active pharmaceutical ingredient for the production of many drugs, in particular gastrodin, which has a wide range of beneficial effects on epilepsy, Alzheimer’s disease, Parkinson’s disease, affective disorders, cerebral ischemia, cognitive disorders.\u0000It is known that 2- and 4-hydroxybenzyl alcohols and mixtures of both compounds are obtained by the interaction of phenol with formaldehyde in the presence of basic catalysts. Due to its high reactivity with formaldehyde, the isolation of pure compounds from the reaction mixtures obtained during the interaction of phenol with formaldehyde is a big problem. Isolation of 2-hydroxybenzyl alcohol in pure form from reaction mixtures is possible only using processes that cannot be carried out on an industrial scale and is accompanied by low yields of the target product. It is possible to get rid of these problems by means of the process of direct oxidation of the 2-hydroxytoluene with ozone in the liquid phase since methods of selective ozonation of methylbenzene to the oxygen derivatives are already known. Therefore, the development of a new low-temperature synthesis of 2-hydroxybenzyl alcohol using ozone is an urgent task.\u0000The aim of the work is to study the reaction of the oxidation of 2-hydroxytoluene by ozone in a solution of a stop reagent and catalytic impurities of compounds of transition metals and mineral acids for the development of a new method of synthesis of 2-hydroxybenzyl alcohol.\u0000Materials and methods. For the experiments, acetic anhydride of p. a. qualification was used; glacial acetic acid of puriss. qualification, which before use was purified by distillation under vacuum in the presence of potassium permanganate, 2-hydroxytoluene of puriss. Qualification, manganese (II) acetate of pur. Qualification, sulfuric and phosphoric acids of puriss. qualification.\u0000To determine the concentration of ozone in the gas phase, a spectrophotometric method was used, based on the measurement of the optical density of the gas flow in the UV region. For this purpose, a spectrophotometer SF-46 LOMO was used, in the measuring chamber of which a flow cuvette with quartz windows was installed. The material of the cuvette was Teflon. Continuous monitoring of the current concentration of ozone, with the recording of the analysis results in the form of a kinetic curve, was carried out when ozone-containing gas passed through the curette at a certain wavelength of a monochromatic light source.\u0000Results. The reaction of oxidation of 2-hydroxytoluene by ozone in a solution of the stop reagent – acetic anhydride was studied. It was shown that in the presence of sulfuric acid, it was possible to carry out direct ozonation of 2-hydroxytoluene to 2-hydroxybenzyl alcohol, which was formed in the kind of 2-acetoxybenzyl acetate with a yield of 13.0 %. The main products of the reaction under these conditions are aliphatic compounds, which are formed after the destruction of the aro","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"101 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77431951","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Methods of synthesis of 1,2,4-triazole derivatives with methoxyphenyl and study the spectrum of their pharmacological activity","authors":"D. Dovbnia, A. Kaplaushenko","doi":"10.14739/2409-2932.2023.1.267174","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.1.267174","url":null,"abstract":"In today’s society, the work of a pharmaceutical worker is very respectful, because it is difficult to imagine the treatment of people without the use of drugs. As time passes, the number of diseases with their own characteristics only increases, so the creation of drugs of synthetic origin remains an actual task for scientists around the world. There are a large number of heterocyclic systems, the derivatives of which exhibit a wide range of pharmacological activities, namely, furan, pyrrole, pyrazole, pyridine, pyrimidine, purine, and many others. Particular attention is drawn to structures that have low toxicity. Undoubtedly, the initial heterocyclic substance must have several reactive centers in order to build the most effective pharmacophores.\u0000Studies by scientists from around the world point to the prospect of using derivatives of the 1,2,4-triazole heterocyclic system as models for new biologically active substances.\u0000The aim of the work was to summarize data on modern methods for the synthesis of 1,2,4-triazole derivatives, to determine the effect of a methoxyphenyl substituent on reactivity and changing the spectrum of pharmacological activity.\u0000Materials and methods. In the work, we used such methods as analytical, information search, descriptive, generalization. The materials of the research were information from the professional literature on the methods of synthesis and study of the biological activity of 1,2,4-triazole derivatives with methoxyphenyl.\u0000Results. A search, analysis, and generalization of information on the methods of synthesis and study of the biological activity of 1,2,4-triazole derivatives with methoxyphenyl were carried out. As a result of the studying available sources and implementation of scientific research, it was found that studies of 1,2,4-triazole derivatives with methoxyphenyl occupy an important place in the Ukrainian pharmaceutical industry, as they have a wide range of pharmacological activity. Also they show low rates of acute toxicity and are perspective to create new APIs on their base\u0000Conclusions. Processing, analysis, systematization, comparison, and generalization of modern sources of information indicate a wide synthetic variability, a fairly wide range of biological activity, and low rates of acute toxicity of 1,2,4-triazole derivatives, with methoxyphenyl at the 5th position of the nucleus of this heterocycle and a wide range of their applications.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86065568","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}