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

{"title":"Analysis of the activity of c-kit immunopositive alpha-cells of the pancreas in exogenous infusions and endogenously formed pathology","authors":"T. Ivanenko","doi":"10.14739/2409-2932.2023.1.273223","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.1.273223","url":null,"abstract":"There are a number of factors and agents that change the population of endocrinocytes and their secretory activity depending on various conditions and experimentally formed pathologies. These include the impact of intermittent hypoxic hypoxia; experimentally formed pathology (diabetes); genetically formed pathology (arterial hypertension), direct effect on endocrinocytes of the pancreas with their own pathophysiological mechanism. In this context, it is interesting to analyze the state of the progenitor potential of alpha cells depending on the living conditions of the organism, its effects, and developing pathological conditions in it.\u0000The aim of the work is to determine the activity of the proliferative factor c-kit in alpha cells under exogenous factors – intermittent hypoxic hypoxia and endogenously formed pathology – arterial hypertension and diabetes.\u0000Materials and methods. The study was conducted on the pancreas of SHR and Wistar rats. Glucagon and c-kit in pancreatic islets were determined by the immunofluorescence method. The immunofluorescence reaction was studied with an AxioImager-M2 fluorescence microscope.\u0000Results. Analysis of the c-kit positive alpha-cell index in rats with diabetes showed a 5-fold increase. This was explained by the fact, that the development of hyperglycemia in diabetes mellitus was characterized not only by an increased level of glucose in the blood due to insufficient insulin production but also due to an increase in the number of alpha cells, their active proliferation and possible transdifferentiation from beta cells. The number of c-kit positive alpha cells in SHR rats decreased. This may indicate that these changes were not so related to a violation of the modulation of the transcription factor, but to the participation of neurogenic mechanisms. The decrease in c-kit positive alpha cells in animals with hypoxic hypoxia can be explained by transdifferentiation (remodeling) changes, aimed at suppressing proliferative processes in alpha endocrinocytes.\u0000Conclusions. The increase in the number of c-kit positive alpha cells in rats with diabetes is explained by the fact, that the development of hyperglycemia in diabetes is characterized not only by an increased level of glucose in the blood due to insufficient insulin production but also by an increase in the number of alpha cells, their active proliferation and possible transdifferentiation from beta cells. A decrease in the number of c-kit positive alpha cells in SHR rats may indicate that these changes are not so much related to a violation of the modulation of the transcription factor, but to the participation of neurogenic mechanisms. The decrease in c-kit positive alpha cells in animals with hypoxic hypoxia can be explained by transdifferentiation (remodeling) changes, aimed at suppressing proliferative processes in alpha endocrinocytes.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"55 27 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81162924","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":"Research of the domestic market of drugs for the treatment of HIV infection","authors":"T. P. Zarichna, T. Brytanova","doi":"10.14739/2409-2932.2023.1.272611","DOIUrl":"https://doi.org/10.14739/2409-2932.2023.1.272611","url":null,"abstract":"The aim of the research is to study the domestic market of medicines for the treatment of HIV infection to optimize the drug supply of the target group of patients.\u0000Materials and methods. Electronic sources of information (State Register of Medicines of Ukraine, Compendium-online, Tabletki.ua) were used to achieve the goal. System-analytical, mathematical-statistical, and comparative methods of analysis were used.\u0000Results. The study of the assortment of drugs for the treatment of HIV infection showed the heterogeneity of the specified segment of the pharmaceutical market of Ukraine: there are solid and liquid dosage forms, both original and generic. The analysis of the company structure made it possible to establish that the national market of drugs for the treatment of HIV infection was dominated by foreign manu­facturers (95.93 %), the largest share of which was pharmaceutical companies from India (67.07 %).\u0000The competitiveness of pharmaceutical firms supplying drugs for the treatment of HIV infection was studied. It was established that the firm Janssen-Silag S.p.A., Italy, occupied the most stable position in the studied market segment. A qualitative analysis of the mentioned medicines was carried out. The most effective and rational of them were determined.\u0000Conclusions. A study of the domestic market of drugs for the treatment of HIV infection was conducted. The assortment and brand structure of this market segment was determined. The level of competitiveness of the above-mentioned pharmaceutical companies were analyzed, and the most successful of them were identified. At the same time, it was established that domestic pharmaceutical companies supply only 4.07 % of drugs of two out of five groups according to the ATS classification to this segment of the market. In connection with this, the development of new drugs of the specified action and the development of their production in Ukraine is important.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"5 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78612321","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":"Search for potential hypoglycemic agents among potassium salts of 3-benzyl-8-substituted xanthines","authors":"K. Aleksandrova, Yevhen S. Pruhlo, Y. Mykhalchenko, O. Shkoda, O. Y. Cherchesova","doi":"10.14739/2409-2932.2022.3.253385","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.253385","url":null,"abstract":"Nowadays, the prevalence of metabolic syndrome (MS) is a serious problem among the world’s population. Metabolic syndrome includes the so-called “deadly” quartet – hypertension, type 2 diabetes mellitus (diabetes mellitus), dyslipidemia and alimentary obesity.\u0000After all, type 2 diabetes is included in the list of pathologies of the metabolic syndrome, it is important to find ways to alleviate the disease. Derivatives of such a heterocyclic system as xanthine are of great interest in this aspect.\u0000The aim of the study was to explore the hypoglycemic activity of newly synthesized water-soluble derivatives of 3-benzyl-8-substituted xanthines.\u0000Materials and methods. We obtained water-soluble potassium 3-benzyl-8-R-xanthin-7-ides, the structure and individuality of which were confirmed by a set of physical-chemical studies.\u0000Results. The hypoglycemic effect of the newly synthesized compounds was assessed by an oral glucose tolerance test. The obtained data were processed using modern statistical in silico-methods.\u0000Conclusions. The results of the hypoglycemic activity study among the potassium salts of 3-benzyl-8-substituted xanthine derivatives showed, that some new compounds are in close vicinity to the reference drug’s hypoglycemic action.\u0000 ","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"24 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72800392","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":"Features of the course urate nephrolithiasis, comorbid with the metabolic syndrome","authors":"A. Hubar, M. A. Dovbysh, O. M. Mischenko, I. M. Dovbysh","doi":"10.14739/2409-2932.2022.3.266616","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.266616","url":null,"abstract":"The aim of the work is to study the peculiarities of the course of urate nephrolithiasis and urate nephrolithiasis comorbid with metabolic syndrome.\u0000Materials and methods. Clinical and laboratory data of 183 patients. The control group of patients with urate nephrolithiasis received traditional therapy. The patients of the main group with urate nephrolithiasis comorbid with metabolic syndrome took quertin and traditional therapy, as well as popular medical drugs that correct metabolic processes. Clinical laboratory, biochemical, ultrasound, radiological, radioisotope, immunoenzymatic, and physical-chemical methods were used.\u0000Results. The pain was more intense in patients with urate nephrolithiasis than in patients with urate nephrolithiasis comorbid with metabolic syndrome. Manifestations of the inflammatory process increased in patients with urate nephrolithiasis comorbid with metabolic syndrome, and concomitant diseases intensified the excretion of stone-forming compounds. Metaphylaxis with quertin against the background of commonly accepted drugs that correct metabolic processes had a positive effect on the course of urate nephrolithiasis comorbid with metabolic syndrome and contributed to the reduction of stone formation relapse.\u0000Conclusions. In-depth diagnosis of metabolic processes can help the doctor to correctly determine the differentiated tactics of examination and treatment, as well as to prevent possible complications in a timely manner.\u0000 ","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"64 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77162013","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":"Comparative study of the specific activity of soft application drugs with vinpocetine","authors":"V. V. Hladyshev, D. Romanina, O. B. Kharaponova, A. V. Kurinnyi, I. V. Hnitko, I. O. Pukhalska, S. A. Hladysheva","doi":"10.14739/2409-2932.2022.3.264032","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.264032","url":null,"abstract":"In modern neurology, the main component of successful treatment of cerebrovascular pathology is pharmacotherapy. At the same time, the arsenal of effective medicines of evidence-based medicine in this area is quite limited. Vinpocetine (Cavinton) is one of the drugs that effectively selectively corrects cerebral perfusion. The use of alternative ways of absorption of vinpocetine (rectal and nasal) in certain soft application dosage forms will allow to significantly increase the bioavailability of the medicinal substance, reduce the level of adverse reactions from its use and expand the pharmacotherapeutic arsenal of domestic effective neuroprotective drugs. Taking into account the above, the employees of the Department of Medicines Technology of Zaporizhzhia State Medical University, on the basis of complex physical-chemical, pharmacotechnological, rheological and biopharmaceutical research, proposed rational formulations and technologies of two new soft application dosage forms of vinpocetine – rectal suppositories on a lipophilic basis and nasal cream on an emulsion basis for the therapy of arterial hypertension of II–III stages with cerebrovascular complications, reduction of the manifestation of neurological and/or mental symptoms in various forms of cerebral blood circulation insufficiency, consequences of a stroke, transient ischemic attack, etc.\u0000The aim of the work is to study the specific activity of the proposed innovative application dosage forms of vinpocetine.\u0000Materials and methods. Nasal ointment containing 0.5 % vinpocetine on an emulsion basis and rectal suppositories with vinpocetine 0.01 g on a lipophilic carrier were used as the object of preclinical studies, which ensure optimal release of the active pharmaceutical ingredient. The study of the specific activity of the developed medicinal forms of vinpocetine was carried out on a model of acute cerebrovascular accident of the type of ischemic stroke. Vinpocetin tablets (Astrapharm, Ukraine), which are used in neurological practice quite effectively and over a long period of time, were used as a comparison drug.\u0000Results. The comparative results showed that the appointment of all studied drugs led to an increase in motor activity. In addition, the administration of medicinal forms of vinpocetine reduced the development of cognitive and cognitive disorders after acute disorders of cerebral blood circulation. It was found that the highest result was shown by the group of animals that received a course of vinpocetine intranasally. In the groups of animals that received vinpocetine for 4 days, markers of oxidative stress – aldehyde phenylhydrazones and ketone phenylhydrazones – were significantly reduced. The highest activity was demonstrated by the pharmaceutical form of vinpocetin, which was used intranasally for 4 days. The introduction of dosage forms of vinpocetine exerted an energizing effect, which was expressed in an increase in the level of macroergic phosphates. Evidently, v","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"7 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83274457","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":"Research of the current state of the market of vitamin and mineral complexes for pregnant women and information support for women during pregnancy","authors":"V. Demchenko, N. Tkachenko, V. Demchenko","doi":"10.14739/2409-2932.2022.3.259188","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.259188","url":null,"abstract":"Aim of the work is to study of the domestic market of vitamin and mineral complexes for pregnant women with the subsequent formation of an information array for making rational decisions on the formation of the pharmacy range of this group of products and information support for women during pregnancy.\u0000Materials and methods. The State Register of Medicinal Products of Ukraine, the Compendium Online Directory of Medicinal Products, Internet resources on drug search in Ukrainian pharmacies GeoApteka and Tabletki.ua, Internet resources of online pharmacies, wholesale offers of vitamin and mineral complexes for pregnant women for pharmacies according to the “Apteka” software package were used as research material. The marketing method, monitoring methods, logical generalization, grouping, and graphic were used in the work.\u0000Results. Based on the analysis of information sources about vitamin and mineral complexes for pregnant women, two assortment groups were formed: 99 % of the segment is represented by special food products and 1 % – by medicines. We studied the corporate structure of the market, as well as analyzed the socio-economic accessibility for consumers – pregnant women.\u0000Conclusions. The Ukrainian pharmaceutical market of vitamin and mineral complexes for pregnant women is dominated by generic multicomponent drugs of foreign production, which have medium availability for the consumer. This situation creates the preconditions for the development of own production of proper quality, which will increase their availability and reduce the economic burden on the consumer – a pregnant woman. The information support of women before the beginning of pregnancy planning and during childbirth is in satisfactory condition. This is primarily due to the need for a woman to see a doctor during pregnancy planning and constant monitoring during pregnancy. On the other hand, pharmaceutical care is not able to compensate for the lack of information on vitamin and mineral complexes for pregnant women due to the peculiarity of the woman’s condition – pregnancy, which requires medical supervision.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90522831","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":"Effectiveness of antiviral treatment of patients with chronic hepatitis C GT 1b depending on the presence of comorbid chronic renal insufficiency","authors":"CD O. V H. V. Venytska B, Riabokon","doi":"10.14739/2409-2932.2022.3.265483","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.265483","url":null,"abstract":"Aim. The aim of the work was to analyze the effectiveness of antiviral therapy (3D mode) in patients with chronic hepatitis C (CHC) GT1 in clinical practice, depending on the presence of comorbid chronic renal insufficiency stage V, who receiving hemodialysis.\u0000Materials and methods. 101 patients with CHC GT1 who received antiviral therapy (AVT) according to the scheme OBV/PTV/r + DSV ± RBV (3D-mode) during 12 weeks were included in the study. All patients with CHC were divided into two groups depending on the presence of comorbid chronic renal insufficiency (CRI): 92 patients who did not have accompanying CRI and 9 patients with comorbid CRI stage V who received program hemodialysis.\u0000Results. The effectiveness of antiviral therapy in patients with CHC GT1 according to the OBV/PTV/r + DSV ± RBV scheme in clinical practice was high in terms of the achievement of 12 weeks sustained virologic response (SVR 12) SVR 12 (94.1 %). The frequency of achieving SVR 12 in CHC patients without concomitant CRI was 94.6 %, and with of comorbid CRI stage V (hemodialysis) – 88.9 % and had not statistically significant differences (P > 0.05). Treatment according to the 3D-mode was accompanied with stable normalization of ALT activity in 86.0 % of patients with CHC, and the frequency of it is achievement did not depend on the presence of comorbid CRI stage V (100.0 % vs. 85.2 % in patients without the specified concomitant pathology, P > 0.05).\u0000Conclusions. The effectiveness of antiviral therapy in patients with CHC GT1 according to the OBV/PTV/r + DSV ± RBV scheme in clinical practice is high in terms of the achievement of SVR 12 (94.1 %) and does not depend in the presence of comorbid CRI stage V in the patient (94.6 % vs. 88.9 %, P > 0.05). The severity of liver fibrosis does not affect the effectiveness of AVT in patients with CHC GT1 in the presence of comorbid CRI stage V and without this comorbid condition.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"74 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75278072","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":"Prognostic value of P-selectin and sST2 in patients with multiple myeloma","authors":"M. Panasenko, B. Samura, S. Dotsenko","doi":"10.14739/2409-2932.2022.3.266453","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.266453","url":null,"abstract":"Cardiac involvement is one of the most important prognostic markers in multiple myeloma. However, prognostic value of novel biomarkers, such as soluble suppression of tumorigenicity 2 (sST2), P-selectin is unknown in multiple myeloma.\u0000The aim of the work was to investigate the additive predictive effects of novel biomarkers P-selectin and sST2 for cardiovascular events of multiple myeloma patients.\u0000Materials and methods. Levels of P-selectin and sST2 were after anticancer treatment in a total of 67 multiple myeloma patients. The median follow-up duration of the censored cases was 14.0 (11.4–19.1) months. A total of 4 deaths occurred during the follow-up period. ELISA method for measurements of circulating level of P-selectin and sST2 was used.\u0000Results. During follow-up, 36 cardiovascular events and 2 deaths unrelated to cardiovascular events were recorded in 18 (26.9 %) patients. During the study, patients were hospitalized 10 times due to cardiovascular disease. At baseline patients with MM and cardiovascular events which appeared during the observation period had higher levels of P-selectin (P < 0.01), sST2 (P = 0,018), compared to patients without cardiovascular events.\u0000Two novel biomarkers, P-selectin and sST2 showed satisfactory predictive performances for one-year cardiovascular events from ROC analysis. Best cut-off values for predicting one-year cardiovascular events were selected (for sST2 – 31.05 ng/ml, with a sensitivity of 71.5 % and a specificity of 89.8 %; for P-selectin – 54.21 ng/ml, with a sensitivity of 69.6 % and a specificity of 86.2 %). The combination of biomarkers had better prognostic properties compared to P-selectin.\u0000Conclusions. In patients with confirmed multiple myeloma, the biomarkers P-selectin and sST2 showed significant prognostic properties in the occurrence of cardiovascular events during 1 year of follow-up.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78621367","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":"Microscopic, submicroscopic characterization of pro- and anti-inflammatory cell phenotypes of the lungs in conditions of experimental allergic inflammation","authors":"S. Popko","doi":"10.14739/2409-2932.2022.3.264993","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.264993","url":null,"abstract":"The aim is to study the microscopic and submicroscopic characteristics of pro- and anti-inflammatory cell phenotypes of the lungs under conditions of experimental allergic inflammation.\u0000Material and methods. We used histological and electron microscopic methods to study the lungs of 48 male guinea pigs in experimental ovalbumin-induced allergic inflammation, simulated by subcutaneous sensitization and subsequent intranasal inhalation with ovalbumin. Submicroscopic changes of respiratory endocrine cells, goblet cells, exocrine bronchiolar cells, mast cells, macrophages, eosinophils, endothelial cells of guinea pigs lungs were determined.\u0000Results. The most significant reactive submicroscopic changes were established on the 23rd and 30th days of observation in the form of an increase in the functional activity of exocrine bronchiolar and goblet cells, as evidenced by the presence of a light nucleus with a predominance of euchromatin, nucleoplasm of low electron-optical density, nucleoli, developed granular endoplasmic reticulum and an increase in the number of goblet cells secretory mucous granules by electron microscopic examination. The revealed ultramicroscopic features of respiratory endocrine cells (an increase in a number of “empty” core dense vesicles), eosinophilic granulocytes (piecemeal degranulation), an increase in the number of mast cells granules, numerous pseudopodia in macrophages are the confirmation of the active participation of these cell phenotypes in the initiation of inflammation during the early period of the allergic inflammatory process in lungs.\u0000Conclusions. A significant reaction of the innate nonspecific and adaptive immunity occurs in airways during the experimental ovalbumin-induced allergic inflammation, consisting primarily of the functional activation of eosinophilic granulocytes, mast cells, and macrophages, as well as an increase in the secretory activity of exocrine bronchiolar cells and goblet cells, which is confirmed by the changes investigated by electron microscopic examination and are accompanied by reactive changes in the vessels of microcirculatory bed.","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"2008 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78891149","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, antimicrobial and antifungal activity of 3-(2-bromophenyl)-5-(alkylthio)-4-phenyl-4H-1,2,4-triazoles","authors":"A. Safonov, O. Panasenko","doi":"10.14739/2409-2932.2022.3.264691","DOIUrl":"https://doi.org/10.14739/2409-2932.2022.3.264691","url":null,"abstract":"To select a molecule that could become a promising pharmacological agent, chemists use already-known heterocyclic bases by adding pharmacologically active groups. One such heterocyclic system is 1,2,4-triazole base, on the basis of which a huge number of biologically active compounds have already been found. It is known that 1,2,4-triazole derivatives show a fairly high antimicrobial and antifungal effect while remaining low-toxic compounds and 5-alkylthio-1,2,4-triazoles exhibit antimicrobial and antifungal activity. Based on the literature search, it can be concluded that 3-(2-bromophenyl)-5-(alkylthio)-4-phenyl-4H-1,2,4-triazoles are insufficiently studied.\u0000The aim of the work was to synthesize and investigate antimicrobial and antifungal activity among 3-(2-bromophenyl)-5-(alkylthio)-4-phenyl-4H-1,2,4-triazoles.\u0000Materials and methods. It was used 5-(2-bromophenyl)-4-phenyl-4H-1,2,4-triazole-3-thiol as a starting substance, which was synthesized by previously described techniques. 3-(2-Bromophenyl)-5-(alkylthio)-4-phenyl-4H-1,2,4-triazoles were obtained by alkylation of the starting thiol with halohenalkanes (according to the first method) and the addition of hydrochloric acid in an alcoholic medium, then subsequent heating in microwave synthesis system (by the second method). To study the antimicrobial and antifungal activity of the newly synthesized 3-(2-bromophenyl)-5-(alkylthio)-4-phenyl-4H-1,2,4-triazoles, the method of serial dilutions was used according to guidelines.\u0000Results. 3-(2-Bromophenyl)-5-(alkylthio)-4-phenyl-4H-1,2,4-triazoles were obtained by two methods: a) an equivalent amount of halohenalkane was added to 5-(2-bromophenyl)-4-phenyl-4H-1,2,4-triazole-3-thiol (I) (solvent – KOH pre-dissolved in 2-propanol). Boiled to pH = 7; b) 5-(2-bromophenyl)-4-phenyl-4H-1,2,4-triazole-3-thiol (I) (solvent – methyl or 1-propyl alcohol and 10 drops of HCl) was heated in Milestone Flexi Wave microwave synthesis system. Reaction conditions: The mixture was heated for 45 minutes at a temperature of 150 °C, a pressure 14.4 bar, ΔMW ≈ 200 W. The completeness of the reaction was determined using a gas chromatograph Agilent 7890B with a mass spectrometric detector 5977B. Antimicrobial and antifungal activity of 3-(2-bromophenyl)-5-(alkylthio)-4-phenyl-4H-1,2,4-triazoles (6 new compounds) was investigated. The most active compound with antifungal and antimicrobial effect was IIi. Substances IIa–IIe had moderate antimicrobial effect.\u0000Conclusions. New 3-(2-bromophenyl)-5-(alkylthio)-4-phenyl-4H-1,2,4-triazoles were synthesized by two methods. The antimicrobial and antifungal activity was investigated for the obtained compounds. The most active compound was 3-(2-bromophenyl)-5-(decylthio)-4-phenyl-4H-1,2,4-triazole (IIi). Some conclusions were drawn regarding the dependence of “structure – antimicrobial and antifungal effect”: the antimicrobial effect increased with the length of the carbon radical; changing the decyl radical to another one in the mol","PeriodicalId":10800,"journal":{"name":"Current issues in pharmacy and medicine: science and practice","volume":"4 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89384493","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}