Andrej Kaplaushenko

Zaporozhye State Medical University | ZSMU · Physicall and colloidal chemistry Department

Ще на світанку відродження української хімічної мови один із її творців – видатний вчений і реформатор науки А.М.Голуб (1918-1977) писав: «Як у коморі хорошого господаря різні речі розташовані по певних полицях і скриньках, так в арсеналі фактів,що ними оперує хімія,неодмінною умовою є раціональна система».....

Ще на світанку відродження української хімічної мови один із її творців – видатний вчений і реформатор науки А.М.Голуб (1918-1977) писав: «Як у коморі хорошого господаря різні речі розташовані по певних полицях і скриньках, так в арсеналі фактів,що ними оперує хімія,неодмінною умовою є раціональна система». Отже, вивчення природи та успішне викорис...

Derivatives of 1,2,4-triazole are actively researched by scientists and synthetic pharmacologists. The last studies have shown that potassium 2-((4-amino-5- (morpholinomethyl)-4H-1,2,4-triazol-3-yl)thio)acetate with low toxicity series exhibits antioxidant and hepatoprotective properties. Therefore, the purpose of this work was to develop a method...

Objective: The aim of this research was to synthesize and evaluate physical-chemical properties of 5-pheneyhyl-4-R-3-thio-1,2,4-triazole and to establish identity and structure of the synthesized compounds, namely alkil-2-((5-phenethyl-4-R-1,2,4-triazole-3-yl)thio)acet(propan,benz)imidates. Methods: As starting materials for synthesis of alkil-2-((...

Objective: The goal of this research was to study fragmentation pathways of series salts of 1,2,4-triazolylthioacetate acids. Methods: The study was done in the Electrospray ionization source with single quadrupole mass spectrometer Agilent 6120 after elution through column Zorbax SB-C18, 30 mm × 4.6 mm, 1.8 μm at Agilent 1260 infinity high-perform...

Ukraine takes the second place in Europe for the dissemination of cancer. Ukrainian pharmaceutical market practically doesn’t have domestic anti-tumor drugs. That’s why, many scientists of pharmaceutical industry work in this direction. The searching of biologically active substances among derivatives of 1,2,4-triazole is actually for today. Anastr...

Relevance of pharmaceuticals with high efficiency and low cost for the prevention and treatment of diseases of the digestive system is unquestionable. It would be appropriate to mention that we carried out an analysis of a number of studies in which hepatoprotective effects of 1,2,4-triazole derivatives were carried out, and showed high hepatoprote...

Diuretic drugs are drugs that, by blocking the transport systems of the renal tubules, promote the removal of excess electrolytes and water from the body, normalization of the internal environment. They eliminate edema, reduce the fluid content in the body cavity. Diuretic drugs differ in their chemical structure, the mechanism of action on the uri...

Today’s a creation of new domestic medicines is very important problem for pharmacy and medicine. Therefore, it is relevant to synthesize new domestic biologically active compounds. It is known that a large number of new 3-thio and 4-amino derivatives on the basis of 1,2,4-triazole have recently been synthesized, among which compounds with high ph...

In order to create new biologically active substances among 1,2,4-triazole derivatives the methods of synthesis of 5-((1H-tetrazol-1-yl)methyl)-4-R-4H-1,2,4-triazole-3-thiols have been proposed and their interaction with halogen nitriles has been studied. The structure of received compounds, namely 2-((5-((1H-tetrazole-1-yl)methyl)-4-R-4H-1,2,4-tri...

p>The results of studies of the effect of Cadmium influence on the state of the enzyme and nonenzyme system of antioxidant protection of young cattle organism, namely on the activity of superoxide dismutase, catalase, glutathione peroxidase, level of reduced glutathione, Selenium, vitamins A and E. It was determined that the feeding of young bulls...

Bile acids play a leading role in the physical and colloidal properties of bile stabilization. Lack of bile acids consequences result in the formation of cholesterol stones in the gall bladder, diarrhea and steatorrhea, fat-soluble vitamins impaired absorption, and kidney stones formation (oxalates). Investigation of altered bile composition, espe...

The wide use of 1,2,4-triazole derivatives in medical practice is primarily explained by two most important properties: high biological activity and low toxicity. It is difficult to overestimate the contribution to medical practice, which such medicines as posaconazole and letrozole have made. Many scientists of the pharmaceutical industry pay atte...

The wide use of 1,2,4-triazole derivatives in medical practice is primarily explained by two most important properties: high biological activity and low toxicity. It is difficult to overestimate the contribution to medical practice, which such medicines as posaconazole and letrozole have made. Many scientists of the pharmaceutical industry pay atte...

Purpose. A development and validation of new sensitive, high efficient and selective HPLC determination method of intermediates technological contaminations in bulk drug of morpholin-4-ium 2-((4-(2-methoxyphenyl)-5-(pyridine-4-yl)-4H-1,2,4-triazole-3-yl)thio)acetate (active pharmaceutical ingredient – API). Materials and methods. LC System was Agi...

The article gives the results of the research on the influence of a developed complex liposomal preparation on the dynamics of morphological and biochemical indicators of the blood of rats subjected to modeled oxidative stress caused by intermuscular injection of 50% carbon tetrachloride at a dose of 0.25 ml per 100 g of body mass. We found that in...

Over the past decade the number of publications, that contain different aspects of chemistry and use of triazoles and tetrazoles have been doubled and continues to grow. Puplications of recent years show that heterocycles with 1,2,3,4-teterazoles and 1,2,4-triazoles are biologically active compounds with a broad spectrum of action. This fact indica...

HPLC-MS-procedure for determination of the active pharmaceutical ingredient of the drug «Avesstym» - morpholine 2-(5-(pyridin-4-yl)-l,2,4-triazol-3-ylthio)acetate in the poultry eggs has been developed; conditions of chromatographing and ESI-MS-detection have been ground, the procedure of sample preparation has been matched. Validation of the devel...

Cancer is one of the main problems of the whole world. Statistics shows that over the past 100 years the level of morbidity and mortality in the world due to the oncopathologies has moved from tenth to second place. It takes next position only after the diseases of the cardiovascular system. According to WHO data, 10 million people get sick per yea...

Scientists around the world pay considerable interest to chemistry of 1,2,4-triazole and 1,2,3,4-tetrazole thanks to the number of valuable properties of this class of compounds. Literary sources indicate that the core of 1,2,4-triazol and 1,2,3,4-tetrazol are fragments of many known drugs and bioactive compounds. Therefore, synthesis, studying phy...

The reactivity of substituted 5,7-dichloro-9-hydrazine acridine that exhibit various pharmacological activity by studying acid-base equilibria in the ethanol-water binary solvent (50 Mol % ethanol) at 25°С using the method of potentiometric titration has been investigated. The values рК of the corresponding conjugate acids obtained for 7 compounds...

A simple, rapid and reproducible isocratic reversed-phase LC-ESI-MS method has been elaborated for determination of the piperidin-1-ium {[5-(2-furyl)-4-phenyl-4H-1,2,4-triazol-3-yl] thio}acetate, active pharmaceutical ingredient (API) of the antiviral veterinary drug "Tryfuzol" in the poultry eggs. The samples were extracted by dimethyl sulfoxide a...

The rapid development of new "civilization diseases" is one of the negative manifestations of modern technological progress. These diseases include obesity, atherosclerosis, allergy, depression and others. Some of them are still difficulty treated. This fact significantly affects the level of human development. The cause of the problem is the lack...

Aim. We have continued the study of 1,2,4-triazole derivatives, which contain 2-, 3- , 4-methoxyphenyl or 3,4,5- methoxyphenyl substituents in 5th position of the triazole nucleus. An acute toxicity has been investigated for 11 eleven different classes of synthesized compounds based on heterocyclic triazole system. Methods. Investigations have bee...

Development of sensitive, acurate, reproducible HPLC-DMD-MS method for determination of the residualamounts of active drug substance "Tryfuzol" in poultryhomogenatesamples and application of this method for testing chiken groups is an important task for the confirmation of thi drug safety. The substance extraction conditions were optimized for meth...

Aim. A number of references of the last ten years have been carefully studied with bibliosemantic method to compile information on the participation of 1,2,4-triazoles in chemical reactions. Introduction of new domestic drugs intopractice, which could compete with expensive imported drugs,is oneof the most important social and economic problem sof...

THE STUDY OF RETENTION REGULARITIES FOR THE POTENTIAL DRUG SUBSTANCES OF 1,2,4-TRIAZOL- 3-YLTHIOACETIC ACIDS AND THEIR SALTS SERIES BY THE METHOD OF HPLC/DAD-MS B.O.Varynskyi, Ye.G.Knysh, V.V.Parchenko, O.I.Panasenko, A.G.Kaplaushenko Key words: retention characteristics; 1,2,4-triazol-3-ylthioacetic acids; HPLC/DMD-MS The derivatives of 1,2,4-tria...

It is known that drugs based on the 1,2,4-triazole have a wide spectrum of biological activities. They are effective cardioprotectors, hepatoprotectors, anti-oxidants, which are widely used in cardiology practice. So this class of heterocyclic compounds has all the attributes of relevance. We have synthesized new 2-(5-(phenoxymethyl)-4-R1-1,2,4-tr...

The search of new biologically active substances, which can be potential drugs with low toxicity and high levels of biological effects, is one of the major aims of modern medicine and pharmacy. Chemical modification of heterocyclic molecules, such as 1,2,4-triazoles derivatives is a promising direction in this problem solving. So modern medicine su...

New salts of 2-(5-(4-methoxyphenyl(3,4,5-trimethoxyphenyl))-1,2,4-triazole-3-ylthio)-acetic acids have been synthesized. The structure has been proven and the physical-chemical properties and actoprotective activity of the synthesized compounds have been studied. The relationship between the structure of the obtained salts and actoprotective activi...

HPLC-MS analysis of 4-amino-5-(4-nitrophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione tautomeric derivatives has been performed and composition of the tautomers mixture has been set. The relationship between the structure of synthesized compounds and their UV-spectrums has been studied, the results of atomic charges calculation have been described....

To find new low-toxic, biologically active compounds, we have synthesized a series of alkylthio(sulfo)derivatives of 1,2,4-triazoles, which contain 2-, 3-, 4-methoxyphenyl or 3,4,5- trimethoxyphenyl substitutes at the C5 atom of 1,2,4-triazole nucleus. The structure of the obtained compounds has been confirmed by complex of modern physical and chem...