Aim. One of the main ways of new biologically active substances search with low toxicity is synthesis of water-soluble compounds. So we developed synthesis methodic of new water-soluble 3-benzyl-8-methylxanthinides-7 by interaction of 3-benzyl-8-methylxanthine with bases in aqueous or aqueous-alcoholic medium.Methods and results. Universal method of obtaining 3-benzyl-8-methylxanthinyl-7-acetic acid, its amide and water-soluble salts has been developed. Also, as example, we offered alternative method of synthesis of 3-benzyl-8-methylxanthinyl-7-acetic acid’s esters. The structure and individuality of synthesized compounds has been proved due by elemental analysis, IR-, 1H NMR-spectroscopy and thin-layer chromatography.
A simple preparative synthetic method for previously undescribed 8-bromo-7-[2-hydroxy-3-(4-tertbutyl) phenoxypropyl-1]-3-methylxanthine derivatives, potential biologically active compounds and convenient synthons for further synthetic investigations, was developed. The spectral properties of the synthesized compounds were studied.
A preparative method for producing of 3-(4′-methylphenyl)-8-methylxanthine, its 7-substituted derivatives, 3-(4′-methylphenyl)-8-methylxanthinyl-7-acetic acid, its ester, amide, hydrazide, ylidenehydrazides, and N-phenylhydrazinocarbothiamide was developed. The structure of the cyclization product of the last, 3-(4′-methylphenyl)-7-[2-(4″-phenyl-5″-thio-4″H-[1″,2″,4″]triazol-3″-yl)methyl]xanthine, was confirmed by elemental analysis and PMR spectroscopy.
Published data on the chemical and physicochemical properties of haloimidazoles are reviewed and classified.
Antimicrobial therapy is a significant element of modern medical and pharmaceutical practice. To create more effective medicines the researches are carried out among different classes of organic substances. One of the key strategies in this field is combination of several pharmacophores in a single molecule. In this aspect, the authors' attention was attracted derivatives xantina, with a wide range of paid activity, and the large variability of the possibility of chemical modification. Objects of the study were derivatives of 3-benzyl-8-methylxanthinyl-7-acetic acid, synthesized by authors' group previously. Antibacterial properties of these compounds were studied on Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa and antifungal activity on Candida albicans. It was found that the most active against Staphylococcus aureus compound was substance A-18, which according to this indicator significantly exceeded the Ampicillin. Compounds A-4, A-9, A-11, A-13, A-19 by antistaphylococcal activity are not inferior to the Ampicillin. Ylidenhydrazide A-16 and S-substituted triazolylmethylxanthines A-22 and A-23 surpassed it. It was also found that hydra-zide A-3, ylidenhydrazides A-6, A-11 A-14 and A-17 showed fungistatic properties comparable to the Nystatin.
Studied NO-simulations of the properties of new 9 synthesized ylidenderivatives hydrazide 3-benzyl-8-methylthioacetic acid on the model of the photoinduced formation of nitric oxide. Study of antioxidant activity showed that in the concentrations 10 -3 mol/l; 10 -5 mol/l; 10 -7 mol/l substances, which have been studied, are NO-simulating the properties of, and performed the quantum-mechanical calculations allow us to attribute the studied substance on the mechanism of action of the group spin traps.
The necessity and grounding of change of some principles in the formation of pedagogical and psychological aspects in teaching of informational technologies are shown. Some peculiarities of information technologies use are described as well as the development of tactic and strategy of the organization of teacher and student cooperative activity.
The presence of an imbalance between energy supply and myocardial needs causes myocardial ischemia. Drugs that can interrupt or reduce the adverse cascade reaction caused by ischemia and the combined name metabolic have a protective effect on the myocardium and have undoubted clinical perspectives. The purpose was to study the cardioprotective properties of new derivatives 3-benzylxanthine (compound A-10, A-12 and A-148) on a model of acute myocardial infarction in rats that simulated Isoprenaline and Pituitrin phased introduction. Cardioprotective activity of the test compounds have been evaluated by reduction of the ST segment on the ECG and reduction of biochemical markers of myocardial ischemic damage and oxidative stress. Test compounds A-10, A-12 and A-148 and the reference preparation Mildronate have been introduced into bioequivalent doses. Estimation of the free-radical oxidation intensity in the myocardium have been determined by markers of oxidative modification of proteins aldehydephenylhydrazones and ketonefephenylhydrazones. About myocardial ischemic injury have been assessed by hyperenzymemia of cardiac isoenzyme Creatine Kinase. Study of cardioprotective properties of new derivatives of 3-benzylxanthine (compounds A-10, A-12 and A-148) have been showed that the test substances may be referred to a cardioprotectors with antioxidant mechanism of action.
The review summarizes and systematizes information reported in literature within a period of 1971 – 2009 about the methods of synthesis and properties of 6-alkyl (aralkyl, aryl, hetaryl)thiopurines and their 9-substitured derivatives.
Published information on methods for the synthesis of haloimidazoles is summarized and classified.