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1,163 result(s) for "Belov, V. V."
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Conformational Landscape, Polymorphism, and Solid Forms Design of Bicalutamide: A Review
Bicalutamide (BCL), a clinically important non-steroidal antiandrogen, exhibits pronounced conformational polymorphism and complex solid-state behaviour that critically influence its physicochemical and biopharmaceutical properties. This review comprehensively integrates current computational and experimental findings on the structural features, polymorphic forms, and intermolecular stabilisation mechanisms of BCL. Key factors, including torsional flexibility, hydrogen-bond networks, π–π stacking, and fluorine–fluorine contacts, are examined with respect to polymorph stability, solubility, and dissolution kinetics. The review also synthesises recent advances in solid-state optimisation strategies—including co-crystals, solvates, amorphous forms, and solid dispersions—and explores the emerging role of supercritical fluid (SCF) technologies in particle engineering and dissolution enhancement. This work offers a framework for designing next-generation BCL solid forms with enhanced bioavailability and stability by connecting molecular insights with formulation approaches.
Conformational Evolution of Bicalutamide in Chloroform: A Comprehensive NMR Study
This study presents new findings on the conformational mobility of the nonsteroidal antiandrogen blocker, bicalutamide, in deuterated chloroform. Based on NOE NMR spectral analysis, quantitative information was obtained regarding the distribution of «open» and «closed» conformer groups in four systems: one with a solid phase (16.7%/83.3%), one without the solid phase (19.7%/80.3%), and two diluted solutions at different concentrations (16.1%/83.9% and 85.3%/14.7%). It was shown that the preparation of molecules for nucleation and the transition to the «closed» conformation occurs at low concentrations and is maintained as the concentration increases until the solid phase is formed. This behavior of conformational evolution contrasts previous understandings of the solid phase’s influence on molecular conformation in solution. The results obtained will offer deeper insights into the conformational evolution of small molecules during nucleation, using bicalutamide as a model.
STARE2: Detecting Fast Radio Bursts in the Milky Way
There are several unexplored regions of the short-duration radio transient phase space. One such unexplored region is the luminosity gap between giant pulses (from pulsars) and cosmologically located fast radio bursts (FRBs). The Survey for Transient Astronomical Radio Emission 2 (STARE2) is a search for such transients out to 7 Mpc. STARE2 has a field of view of 3.6 steradians and is sensitive to 1 millisecond transients above ∼300 kJy. With a two-station system we have detected and localized a solar burst, demonstrating that the pilot system is capable of detecting short duration radio transients. We found no convincing non-solar transients with duration between 65 s and 34 ms in 200 days of observing, limiting with 95% confidence the all-sky rate of transients above ∼300 kJy to <40 sky−1 yr−1. If the luminosity function of FRBs could be extrapolated down to 300 kJy for a distance of 10 kpc, then one would expect the rate to be ∼2 sky−1 yr−1.
Pre-harvest sprouting resistance and haplotype variation of ThVp-1 gene in the collection of wheat-wheatgrass hybrids
The germplasm collection of 87 wheat-wheatgrass hybrids developed in Tsitisin Main Botanical Garden (Russia, Moscow) was evaluated for resistance to pre-harvest sprouting (PHS) by spike sprouting (SS) and germination index (GI) assays as well as for spike and grain features. The PHS resistance variation and haplotype polymorphism of the wheatgrass ThVp-1 and wheat TaVp-1B genes orthologues of Vp-1 was revealed in the studied collection. Four haplotypes of ThVp-1 were revealed: ThVp-1a (41% of the entries), ThVp-1b (13%), ThVp-1c (29%), and ThVp-1d (15%). The association between the allelic state of ThVp-1 and PHS resistance in the wheat-wheatgrass hybrids was shown: haplotype ThVp-1d of the wheatgrass Vp-1 gene is significantly associated with reduced PHS in the wheat-wheatgrass hybrids (mean SS 0.33, mean GI 0.64). The resistant entries may be perspective as a source of PHS resistance in the development of commercial cultivars of perennial wheat.
Germany’s Relations with China: An Uneasy Trinity of Partnership, Competition, and Rivalry
Since 2019, Brussels and Berlin have been building relations with Beijing in the paradigm of a contradictory triad of partnership, economic competition, and systemic rivalry. The current German government continues to adhere to this approach, which was enshrined in the coalition agreement. On its basis, during 2022 and the first half of 2023, the foundations of a Strategy for Relations with China were being prepared, which became the first in the history of Germany and reflected not so much the unity as the differences of the coalition parties in shaping the current Chinese vector of the German state’s foreign policy. As in other strategic issues, the Social Democrats, Greens, and Liberals had to follow the path of compromise, which from the very beginning called into question the possibility of achieving the set strategic goals and objectives in the long term. This article analyzes the features of the preparation of the Chinese strategy of the Federal Government, its adoption, and the implementation of the political and economic provisions formulated in it starting from the second half of 2023. Special attention is paid to the study of the latest trends in foreign trade and investment cooperation between Germany and China in 2023–2024, as well as to the role of various government departments and the European Commission in the development of bilateral relations. The effect of the visits of the Federal Chancellor and Vice Chancellor to China in April and June 2024, which took place against the background of the aggravation of economic relations between Brussels and Beijing, is analyzed. The stumbling block was the issue of state support for Chinese business, which, from the point of view of the European Commission, distorts market competition, giving an unreasonable advantage to Chinese companies. The author attempts to predict the future of Germany–China relations in the context of the formulated triad.
Algorithm for the Reconstruction of the Ground Surface Reflectance in the Visible and Near IR Ranges from MODIS Satellite Data with Allowance for the Influence of Ground Surface Inhomogeneity on the Adjacency Effect and of Multiple Radiation Reflection
An atmospheric correction algorithm is proposed for the reconstruction of the ground surface reflectance from the data of satellite measurements. A distinctive feature of the algorithm is that it takes into account the influence of the ground surface inhomogeneity on the adjacency effect and additional illumination of the ground surface by reflected radiation. These factors are important for the reconstruction of the reflectance of ground surface fragments with sharp reflectance changes and high atmospheric turbidity. The algorithm is based on Monte Carlo programs developed by the authors. To reduce the computing time, we have proposed some original criteria and approaches. To estimate the capabilities of the developed algorithm, its results have been validated by comparing with the results of the MOD09 algorithm for four MODIS bands and measurements for the Portugal surface fragment with coordinates 38.829 N, 8.791 W. Good agreement of the results obtained by the proposed algorithm with the surface measurements and the data obtained by the MOD09 algorithm demonstrates the efficiency of the proposed algorithm in the reconstruction of the ground surface reflectance.
Conformational Screening of Arbidol Solvates: Investigation via 2D NOESY
Understanding of the nucleation process’s fundamental principles in saturated solutions is an urgent task. To do this task, it is necessary to control the formation of polymorphic forms of biologically active compounds. In certain cases, a compound can exist in a single polymorphic form, but have several solvates which can appear in different crystal forms, depending on the medium and conditions of formation, and show different pharmaceutical activity. In the present paper, we report on the analysis of Arbidol conformational preferences in two solvents of different polarities—deuterated chloroform and dimethyl sulfoxide—at 25 °C, using the 2D NOESY method. The Arbidol molecule has various solvate forms depending on the molecular conformation. The method based on the nuclear Overhauser effect spectroscopy was shown to be efficient in the analysis of complex heterocyclic compounds possessing conformation-dependent pseudo-polymorphism. It is one of the types of polymorphism observed in compounds forming crystal solvates. Combined use of NMR methods and X-ray data allowed determining of conformer populations of Arbidol in CDCl3 and DMSO-d6 which were found to be 8/92% and 37/63%, respectively. The preferred conformation in solution is the same that appears in stable crystal solvates of Arbidol.
A fast radio burst associated with a Galactic magnetar
Since their discovery in 2007 1 , much effort has been devoted to uncovering the sources of the extragalactic, millisecond-duration fast radio bursts (FRBs) 2 . A class of neutron stars known as magnetars is a leading candidate source of FRBs 3 , 4 . Magnetars have surface magnetic fields in excess of 10 14 gauss, the decay of which powers a range of high-energy phenomena 5 . Here we report observations of a millisecond-duration radio burst from the Galactic magnetar SGR 1935+2154, with a fluence of 1.5 ± 0.3 megajansky milliseconds. This event, FRB 200428 (ST 200428A), was detected on 28 April 2020 by the STARE2 radio array 6 in the 1,281–1,468 megahertz band. The isotropic-equivalent energy released in FRB 200428 is 4 × 10 3 times greater than that of any radio pulse from the Crab pulsar—previously the source of the brightest Galactic radio bursts observed on similar timescales 7 . FRB 200428 is just 30 times less energetic than the weakest extragalactic FRB observed so far 8 , and is drawn from the same population as the observed FRB sample. The coincidence of FRB 200428 with an X-ray burst 9 – 11 favours emission models that describe synchrotron masers or electromagnetic pulses powered by magnetar bursts and giant flares 3 , 4 , 12 , 13 . The discovery of FRB 200428 implies that active magnetars such as SGR 1935+2154 can produce FRBs at extragalactic distances. Observations of the fast radio burst FRB 200428 coinciding with X-rays from the Galactic magnetar SGR 1935+2154 indicate that active magnetars can produce fast radio bursts at extragalactic distances.
High Precision Human Skin Temperature Fluctuations Measuring Instrument
This paper describes the experimental results of testing a prototype of a high precision human skin rapid temperature fluctuations measuring instrument. Based on the author’s work, an original circuit solution on a miniature semiconductor diode sensor has been designed. The proposed circuitry provides operation in the full voltage range with automatic setting and holding the operating point, as well as the necessary slope of the conversion coefficient (up to 2300 mV/°C), which makes it possible to register fast temperature oscillations from the surface of the human body and other biological objects. Simulation results in the Microcap 12 software and laboratory tests have confirmed all declared design specifications: temperature resolution of 0.01 °C, transducer thermal time constant of 0.05 s. An original thermostat and an experimental setup for the simultaneous registration of the electrocardiogram, pulse wave signals from the Biopac polygraph MP36 and a signal of temperature oscillations from the prototype thermometer have been designed for further investigations. The preliminary test results indicates that using the designed measuring instrument gives a possibility to provide an in-depth study of the relationship between micro- and macro-blood circulations manifested in skin temperature fluctuations.
In vitro renal calculi destruction by a high-frequency glow discharge plasma
Despite the progress made in the treatment of nephrolithiasis, the existing methods of renal calculi destruction are not ideal and have both advantages and disadvantages. Considering the process of high-frequency glow discharge formation on the surface of an electrode and in an electrolyte solution, we obtained the results on the destruction of renal calculi in vitro. It was shown that the destruction of kidney stones by glow discharge plasma was caused by several processes—the plasma induced effect of hydrated electrons and shock wave effect of the electrolyte stimulated by electrical breakdowns in the plasma. The plasma generation modes were configured by estimating the thickness of the vapor–gas layer in which the plasma burns. Thus, the average rate of contact destruction of renal calculi was measured depending on the plasma generator input power and time of plasma exposure. We conclude that the method of stone fragmentation by high-frequency electrolyte plasma is rather perspective and can be used in endoscopic urology for percutaneous and transurethral lithotripsy.