THE STUDY OF SOME PROMISING PHARMACEUTICAL COMPOSITIONS WITH UREASE INHIBITORY ACTIVITY FOR THE TUBERCULOSIS REACTIVATION PREVENTION

Introduction. The aim of the study was to study the ability to inhibit urease by some pharmaceutical compositions that are promising in the prevention of tuberculosis reactivation . In particular, according to a number references sources, quercetin is able to successfully inhibit urease by a non-competitive mechanism. Another compound - dipyrone (metamizol sodium) according to preliminary molecular modeling has a pharmacophore structure similar to urea. Materials and methods. The biochemical studies (urease activity) of some substances effect on urease was carried out. As the leader substances – inhibitors was used quercetin and metamizole, another substances are not shown inhibition activity on the urease. As the substrate a 0.5% aqueous urea solution was used. The reaction was carried out at a temperature of 37 ° C, the incubation time was 10 minutes. The activity of urease was determined by the color reaction with the hypochlorite reagent. Photometry was performed on a FEK-3M photoelectric colorimeter at a wavelength of 590 nm. Results and discussion. Quercetin and metamizole sodium have the strongest inhibitory properties for urease, since the lowest values of semi-inhibitory concentrations are obtained for them. In the presence of chlorophyllipt, the inhibitory activity of quercetin against urease is not suppressed. Metformin showed no inhibitory activity against urease, and it was low for other substances. Conclusion. The highest anti-urease activity showed a composition based on metamizole sodium and quercetin, a little less - based on quercetin and vitamin D. Also interesting for further research is the composition of quercetin and chlorophyllipt

Influence of the inert and active ion bombardment on structure of the transition metal thin films

The results of the experimental research of the inert (He, Ne, Ar, Kr, Xe) and active (O, N) ion impact on the transition metal structure are presentedyesBelgorod State Universit

Forward observables at RHIC, the Tevatron run II and the LHC

We present predictions on the total cross sections and on the ratio of the real part to the imaginary part of the elastic amplitude (rho parameter) for present and future pp and pbar p colliders, and on total cross sections for gamma p -> hadrons at cosmic-ray energies and for gamma gamma -> hadrons up to sqrt(s)=1 TeV. These predictions are based on a study of many possible analytic parametrisations and invoke the current hadronic dataset at t=0. The uncertainties on total cross sections, including the systematic theoretical errors, reach 1% at RHIC, 3% at the Tevatron, and 10% at the LHC, whereas those on the rho parameter are respectively 10%, 17%, and 26%.Comment: 11 pages, 2 figures, LaTeX, presented at the Second International "Cetraro" Workshop & NATO Advanced Research Workshop "Diffraction 2002", Alushta, Crimea, Ukraine, August 31 - September 6, 200

Premartensitic Transition in Ni2+xMn1-xGa Heusler Alloys

The temperature dependencies of the resistivity and magnetization of a series of Ni2+XMn1-XGa (X = 0 - 0.09) alloys were investigated. Along with the anomalies associated with ferromagnetic and martensitic transitions, well-defined anomalies were observed at the temperature of premartensitic transformation. The premartensitic phase existing in a temperature range 200 - 260 K in the stoichiometric Ni2MnGa is suppressed by the martensitic phase with increasing Ni content and vanishes in Ni2.09Mn0.91Ga composition

Crystal and molecular structure of two insecticides: Amido-o, s-dimethylthiophosphate and n-acetamido- o, s-dimeth ylthiophosphate

The crystal and molecular structure of title compounds have been determined by means of X-ray analysis. The amido-O.S-dimethylthiophosphate (1) crystallizes in the monoclinic space group P21/n with cell dimensions a = 5. 374(3), b = 9. 220(4), c = 13.847(5) Å and β = 101.08(5)° at the - 100°C. The N-acetamido-O.S-dimethylthiophosphate (2) crystallizes in the monoclinic space group P21/c with cell dimensions a = 11. 547(3), b = 8. 545(2), c = 8.954(5) Å and β = 93.03(4)°. The structures were solved by direct methods and refined by least-squares to R = 0. 0493(1) and 0.0482(2). The coordination around P of the molecules (1) and (2) is distorted tetrahedrally. Molecules have nearly planar moieties HCSP=O and HNPOC (1), HCSP=O and HCC (0) NHPOC (2) with trans-orientation HCSP, CSP=O and NPOC groups. The angle between these planes is 85.3° (1) and 90.3° (2). There are intermolecular P=O … H-N hydrogen bonds in the crystal structures (1) and (2). © 1991 Taylor & Francis Group, LLC. All rights reserved

New opportunities in the treatment of asthenic symptoms after a new coronavirus infection

Introduction. Asthenia is an urgent problem during the pandemic of new coronavirus infection (COVID-19) because of its high frequency regardless of the severity of the disease.The purpose of this subanalysis of data from the multicenter controlled randomized clinical trial TONUS was to evaluate the efficacy and safety of meldonium therapy for аsthenia in COVID-19 survivors.Materials and methods. A total of 880 patients with asthenia who underwent COVID-19 within the last 6 months were included in the analysis. The efficacy of asthenia therapy was assessed by the MFI-20 scale, Schulte tables, and the General Clinical Impression (CGI) scale. All patients were previously randomized in two parallel branches of the TONUS study, including patients without concomitant disease in TONUS-1 (who received meldonium 500 mg/day for 14 days in the main group) and patients with cardiovascular or cerebrovascular disease in TONUS-2, who received meldonium at a dose of 1000 mg/day for 42 days in the main group. In both arms of the study, the drugs in the comparison groups were multivitamin complexes.Results. For the TONUS-1 groups.In the group of patients receiving meldonium compared with the control group (p < 0.001): total MFI-20 score decreased and was 31 (25; 40); MFI-20 –35 (–46; 23); performance value –5 (–11; –2) seconds; proportion of patients with significant improvement (by CGI-I) by the end of follow-up was 92.8%. For TONUS-2 groups.In the group of patients receiving meldonium compared with the control group (p < 0.001): total MFI-20 score decreased to 35 (27; 44); MFI-20 –34 (–46; –21), performance value –5 (–11; –2), proportion of patients with significant improvement (by CGI-I) by end of follow-up – 90.8%.Conclusion. Significant positive dynamics and regression of asthenia were noted in the groups of patients receiving meldonium in comparison with the control groups

Neuroprotective effects of the novel ethylthiadiazole derivatives (LHT 4-15) in male rats

The study was performed on male rats of the Wistar line. The animals were simulated with total cerebral ischemia with preliminary administration of LHT 4-15 compounds in doses of 25 and 50 mg/kg for 60 min. The data obtained from the neurological deficit and in the behavioral tests of the experimental groups confirm the theory of the presence of ethylthiadiazole derivatives under the LHT code 4–15 neuroprotective properti