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Structural modification of the 1,2,4-triazole core as a strategy for the design of biologically active compounds (literature review)

Thu, 01 Jan 2026 00:00:00 GMT

Название: Structural modification of the 1,2,4-triazole core as a strategy for the design of biologically active compounds (literature review) Авторы: Dovbnia, D. V.; Kaplaushenko, A. H.; Panasenko, O. I.; Panasenko, M. O.; Salionov, V. O.; Ihnatova, T.; Georgiev, K.; Slavov, I.; Довбня, Дмитро Віталійович; Каплаушенко, Андрій Григорович; Панасенко, Олександр Іванович; Панасенко, Марія Олександрівна; Саліонов, Володимир Олександрович Аннотация: The aim. The aim of this review article is to systematize and summarize current literature data on methods of chemical modification of 1,2,4-triazole derivatives, as well as to analyze the impact of structural transformations on their biological activity and pharmacological potentia l. Materials and methods. The analysis was based on scientific publications by domestic and international authors devoted to the synthesis, functionalization, and biological evaluation of 1,2,4-triazole derivatives. Data generalization was carried out using methods of systematic analysis, comparative assessment of synthetic approaches, and analysis of the results of in silico, in vitro, and in vivo studies (molecular docking, ADME analysis, SAR evaluation). Results. It has been shown that 1,2,4-triazole derivatives are characterized by high chemical lability and the ability to undergo modification at the sulfur atom, amino group, and nitrogen atoms of the heterocyclic core. Alkylation and acylation reactions, salt formation, hybridization with other pharmacophoric fragments, as well as the application of microwave-assisted synthesis enable the development of compounds with a wide spectrum of biological activity. Among the studied derivatives, compounds exhibiting antioxidant, antimicrobial, antitumor, anti-inflammatory, neuroprotective, and hypoglycemic activities have been identified. A correlation between the chemical structure of the compounds, the nature of substituents, and their pharmacological properties has been established. Conclusions. 1,2,4-Triazole derivatives represent a promising pharmacophoric platform for the development of new biologically active compounds. Further targeted investigation of their chemical modification pathways and structure-activity relationships offer broad opportunities for the design of potential therapeutic agents.

The Influence of Basic Therapy and New Drugs on NO-Dependent Mechanisms of Cardiac Destruction in Chronic Heart Failure

Thu, 01 Jan 2026 00:00:00 GMT

Название: The Influence of Basic Therapy and New Drugs on NO-Dependent Mechanisms of Cardiac Destruction in Chronic Heart Failure Авторы: Belenichev, I. F.; Popazova, O. O.; Goncharov, O.; Bukhtiyarova, N. V.; Ryzhenko, V. P.; Semenov, D. M.; Oliynyk, S.; Petakh, P.; Kamyshnyi, O.; Бєленічев, Ігор Федорович; Попазова, Олена Олександрівна; Бухтіярова, Ніна Вікторівна; Риженко, Віктор Павлович; Семенов, Денис Михайлович Аннотация: Chronic heart failure (CHF) remains a leading cause of global mortality, characterized by profound molecular and biochemical disturbances, including nitric oxide (NO) system dysfunction, mitochondrial impairment, and oxidative stress. While standard therapies such as ACE inhibitors, SGLT2 inhibitors, and beta-blockers address clinical symptoms, their capacity to interrupt the underlying biochemical mechanisms of cardiomyopathy is often limited. This review examines the pathophysiological role of impaired NO production and reactive oxygen species (ROS) accumulation in exacerbating myocardial contractile dysfunction and disease progression. Special focus is directed toward the development of next-generation β1-blockers with multifunctional properties, including antioxidant, NO-mimetic, and antiapoptotic effects. Evidence suggests that the novel compound Hypertril (1-(β-phenylethyl)-4-amino-1,2,4-triazolium bromide) exhibits significant cardioprotective potential. Experimental data indicate that Hypertril improves eNOS/iNOS expression and enhances NO bioavailability more effectively than conventional β-blockers, leading to stabilized ECG parameters and restored energy metabolism. These findings underscore the clinical relevance of developing NO-mimetic agents to optimize the pharmacological management of CHF.

Аналіз ефективності лікування гонартрозу блокатором інтерлейкіну-1 діацереїном

Wed, 01 Jan 2025 00:00:00 GMT

Название: Аналіз ефективності лікування гонартрозу блокатором інтерлейкіну-1 діацереїном Авторы: Федорова, Олена Петрівна; Пахомова, Світлана Петрівна; Світлицька, О. А.; Бурлака, Кристина Анатоліївна; Устінова, С. О.; Кікнадзе, Т. І.; Fedorova, O. P.; Pakhomova, S. P.; Svitlytska, O. A.; Burlaka, K. A.; Ustiniva, S. O.; Kiknadze, T. I. Аннотация: The aim of the study is to assess the efficacy and safety of the IL-1 blocker diacerein in patients with primary gonarthrosis. Materials and methods: 56 patients aged 54 to 68 years (32 women and 24 men) with a diagnosis of "Primary gonarthrosis" were treated. The study of laboratory parameters revealed an increase in ESR (26±2.1 mm/h), CRP (8.4±1.09 mg/l). The intensity of the pain syndrome was assessed using the visual analog pain scale (VAS), functional insufficiency was assessed using the WOMAC questionnaire (Western Ontario and McMaster University Osteoarthritis Index), and the degree of exacerbation was assessed using the Leken index. Patients received chondroprotectors (glucosamine sulfate at a dose of 400 mg intramuscularly 3 times a week (Dona)) and 200 mg of chondroitin sulfate sodium intramuscularly (Staurum)), a total of 6 injections. The first group (control) included 23 patients who were additionally administered diclofenac sodium intramuscularly at a dose of 75 mg daily, the second group consisted of 23 patients who received diacerein at a dose of 50 mg orally. Results. Before the start of treatment, the pain assessed by patients using VAS in the main group was 78.8±1.77 mm, at the end of treatment - 30.9±1.66 mm (p<0.05). In the control group, the pain level was 75.6±3.56 mm and 32.1±2.54 mm (p<0.05), respectively. At the same time, patients noted both a decrease in starting pain and pain during physical activity. The reduction in pain and an increase in the amplitude of movements in the joint led to a positive dynamics of the total WOMAC index, the value of which decreased significantly more in the group receiving additional diacerein. After a course of therapy in the main group, this indicator was significantly lower compared to the control group. Conclusions. diacerein can be considered in the treatment regimen for primary osteoarthritis in patients who are contraindicated for nonsteroidal antiinflammatory drugs.

Prospects for the Rapid Delivery of Active Pharmaceutical Ingredients to the Brain for Neuroprotective Action: Examples of Nasal Gel Formulations

Thu, 01 Jan 2026 00:00:00 GMT

Название: Prospects for the Rapid Delivery of Active Pharmaceutical Ingredients to the Brain for Neuroprotective Action: Examples of Nasal Gel Formulations Авторы: Belenichev, I. F.; Aliyeva, O. G.; Burlaka, B. S.; Bukhtiyarova, N. V.; Shabelnyk, K. P.; Бєленічев, Ігор Федорович; Алієва, Олена Геннадіївна; Бурлака, Богдан Сергійович; Бухтіярова, Ніна Вікторівна; Шабельник, Костянтин Петрович