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 1-10    11-15 
1.
Инвентарный номер: нет.
   


   
    Combined in silico, ex vivo, and in vivo assessment of L-17, a thiadiazine derivative with putative neuro-and cardioprotective and antidepressant effects / A. Sarapultsev, P. M. Vassiliev, D. M. Grinchii [et al.] // International journal of molecular sciences. - 2021. - Vol. 22, № 24. - P13626
Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ
Кл.слова (ненормированные):
TREATMENT-RESISTANT DEPRESSION -- POST-STROKE DEPRESSION -- C-FOS IMMUNOHISTOCHEMISTRY -- BINDING AFFINITY
Аннотация: Depression associated with poor general medical condition, such as post-stroke (PSD) or post-myocardial infarction (PMID) depression, is characterized by resistance to classical antidepressants. Special treatment strategies should thus be developed for these conditions. Our study aims to investigate the mechanism of action of 2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide (L-17), a recently designed thiadiazine derivative with putative neuro- and cardioprotective and antidepressant-like effects, using combined in silico (for prediction of the molecular binding mechanisms), ex vivo (for assessment of the neural excitability using c-Fos immunocytochemistry), and in vivo (for direct examination of the neuronal excitability) methodological approaches. We found that the predicted binding affinities of L-17 to serotonin (5-HT) transporter (SERT) and 5-HT3 and 5-HT1A receptors are compatible with selective 5-HT serotonin reuptake inhibitors (SSRIs) and antagonists of 5-HT3 and 5-HT1A receptors, respectively. L-17 robustly increased c-Fos immunoreactivity in the amygdala and decreased it in the hippocampus. L-17 dose-dependently inhibited 5-HT neurons of the dorsal raphe nucleus; this inhibition was partially reversed by the 5-HT1A antagonist WAY100135. We suggest that L-17 is a potent 5-HT reuptake inhibitor and partial antagonist of 5-HT3 and 5-HT1A receptors; the effects of L-17 on amygdaloid and hippocampal excitability might be mediated via 5-HT, and putatively mediate the antidepressant-like effects of this drug. Since L-17 also possesses neuro- and cardioprotective properties, it can be beneficial in PSD and PMID. Combined in silico predictions with ex vivo neurochemical and in vivo electrophysiological assessments might be a useful strategy for early assessment of the efficacy and neural mechanism of action of novel CNS drugs.

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2.
Инвентарный номер: нет.
   


   
    Pyrrolylquinoxaline-2-one derivative as a potent therapeutic factor for brain trauma rehabilitation / E. A. Dutysheva, M. A. Mikeladze, N. D. Aksenov [и др.] // Pharmaceutics. - 2020. - Vol. 12, № 5. - С. 414
Кл.слова (ненормированные):
APOPTOSIS -- CEREBROSPINAL FLUID -- HSP70 -- SMALL MOLECULE -- TRAUMATIC BRAIN INJURY
Аннотация: Traumatic brain injury (TBI) often causes massive brain cell death accompanied by the accumulation of toxic factors in interstitial and cerebrospinal fluids. The persistence of the damaged brain area is not transient and may occur within days and weeks. Chaperone Hsp70 is known for its cytoprotective and antiapoptotic activity, and thus, a therapeutic approach based on chemically induced Hsp70 expression may become a promising approach to lower post-traumatic complications. To simulate the processes of secondary damage, we used an animal model of TBI and a cell model based on the cultivation of target cells in the presence of cerebrospinal fluid (CSF) from injured rats. Here we present a novel low molecular weight substance, PQ-29, which induces the synthesis of Hsp70 and empowers the resistance of rat C6 glioma cells to the cytotoxic effect of rat cerebrospinal fluid taken from rats subjected to TBI. In an animal model of TBI, PQ-29 elevated the Hsp70 level in brain cells and significantly slowed the process of the apoptosis in acceptor cells in response to cerebrospinal fluid action. The compound was also shown to rescue the motor function of traumatized rats, thus proving its potential application in rehabilitation therapy after TBI.

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3.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis and Antitubercular Evaluation on Novel 1-Ethyl-5-(hetero)aryl- 1,6-dihydropyrazine-2,3-dicarbonitriles and 3-Cyano-1-ethyl-5-(hetero) aryl-2(1H)-pyrazinones / M. A. Kravchenko, E. V. Verbitskiy, S. N. Skornyakov, P. A. Slepukhin, G. L. Rusinov, O. N. Chupakhin, V. N. Charushin // Anti-Infective Agents. - 2016. - Vol. 14, № 2. - С. 139-144
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PYRAZINES -- ANTITUBERCULOSIS ACTIVITY -- 2(1H)-PYRAZINONE
Аннотация: A simple method based on hydrolysis of 2,3-dicyanopyrazinium salts has been used for the synthesis of the corresponding 5-(hetero)aryl-3-cyano-1-ethyl-2(1H)-pyrazinones. Also, the series of novel 1-ethyl-5-(hetero)aryl-1,6-dihydropyrazine-2,3-dicarbonitriles have been obtained through reduction of the same pyrazinium salts with triethylsilane. The obtained compounds proved to be active in micromolar concentrations in vitro against Mycobacterium tuberculosis H37Rv, Mycobacterium avium, Mycobacterium terrae, as well as against rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis. The data for acute in vivo toxicity in mice have been obtained for these compounds which appear to be promising antitubercular agents

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4.
Инвентарный номер: нет.
   
   T 44


   
    The impact of immunomodulator compound from the group of substituted thiadiazines on the course of stress reaction [Electronic resource] / P. Sarapultsev, O. N. Chupakhin, S. Medvedeva, E. A. Mukhlynina, S. A. Brilliant, L. P. Sidorova, I. Danilova, A. Sarapultsev // International Immunopharmacology. - 2015. - Vol. 25, № 2. - С. 440-449. - Bibliogr. : p. 447-449 (101 ref)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
STRESS -- THIADIAZINES -- L-17 COMPOUND
Аннотация: A significant role of the stress response to many different diseases prompted a search for new specialized and non-specialized anti-stress agents. This study examines the effect of the compound L17 from the group of 5-phenyl substituted-6H-1,3,4-thiadiazine-2-amines, on the manifestations of the stress response. The authors used a standard model of immobilization stress, in which an animal was immobilized on its back for 6 ha day. Parameters of the morphological and functional states of the organs studied were measured and biochemical and enzyme-immunoassays were carried out on the first and second days. This study reveals that the main mechanism by which the L17 compound mediates of its anti-stress was by activation of macrophages on the second day of the experiments and the inhibition of apoptosis in the thymus. The results enable us to suggest that the compound L17 does not improve resistance to stress; however, it does lower the reaction to stress.

\\\\expert2\\nbo\\International Immunopharmacology\\2015. V. 25, N 2. P. 440-449.pdf
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5.
Инвентарный номер: нет.
   
   I-61


   
    Inhibitory activity of fluorine-containing quaternary ammonium salts comprising an N-methylpiperazinyl moiety [Electronic resource] / T. I. Gorbunova, D. N. Bazhin, A. Ya. Zapevalov, V. I. Saloutin // Russian Journal of Applied Chemistry. - 2013. - Vol.86, №7. - С. 992-996. - Bibliogr. : p. 995-996 (21 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
QUATERNARY AMMONIUM SALTS -- N-METHYLPIPERAZINYL -- HYDROCHLORIC ACID CORROSION
Аннотация: New fluorine-containing quaternary ammonium salts comprising an N-methylpiperazinyl moiety, which exhibited a high inhibiting capacity against hydrochloric acid corrosion of low-carbon steel, were synthesized. The polarization-resistance method was applied to determine the uniform corrosion rate of steel-3 in relation to the structure and concentration of the fluorine-containing substituents in the salts. It was found that the structure of the fluorine-containing moiety of the quaternary ammonium salts does not significantly influence the corrosion processes

\\\\expert2\\nbo\\Russian Journal of Applied Chemistry\\2013, v. 86, N 7, p. 992.pdf
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6.
Инвентарный номер: нет.
   
   N 10


   
    N-(2-(2-Pyridyl)ethyl)chitosan (PEC) for Pd(II) and Pt(IV) sorption from HCl solutions / L. A. Santos Sorena, M. Ruiz, A. V. Pestov, A. M. Sastre, Yu. G. Yatluk, E. Guibal // Cellulose. - 2011. - Vol. 18, № 2. - С. 309-325
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
CHITOSAN – PYRIDYL GROUPS -- PALLADIUM -- PLATINUM
Аннотация: Chitosan was modified by grafting 2-pyridyl-ethyl moieties on the biopolymer backbone for the synthesis of a Platinum Group Metal (PGM) sorbent. The sorbent was tested for Pd(II) and Pt(IV) sorption from HCl solutions. Stable for HCl concentrations below 0.5 M, the sorbent reached sorption capacities as high as 3.2 and 2.6 mmol metal g?1 for Pd(II) and Pt(IV), respectively. Metal sorption mainly proceeds by electrostatic attraction in acidic solutions, though a contribution of complexation mechanism cannot be totally rejected. The resistance to intraparticle diffusion is the main controlling mechanism for uptake kinetics. While agitation speed has a limited effect on kinetics, metal concentration and sorbent dosage have a greater effect on the kinetic profiles. The intraparticle diffusivity varies between 3 ? 10?11 and 4.5 10?10 m2 min?1. Thiourea (combined with HCl solution) is used for Pd(II) and Pt(IV) desorption. The resin could be desorbed and recycled for a minimum of five cycles maintaining high efficiencies of sorption and desorption. ??

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7.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis and inhibiting capacity of new fluorine-containing quaternary ammonium salts / T. I. Gorbunova, D. N. Bazhin, A. Ya. Zapevalov, V. I. Saloutin // Russian Journal of Applied Chemistry. - 2011. - Vol.84, №6. - С. 972-977
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
SYNTHESIS -- INHIBITING CAPACITY -- AMMONIUM SALTS
Аннотация: New fluorine-containing quaternary ammonium salts exhibiting a high inhibiting capacity against hydrochloric acid corrosion of low-carbon steels were synthesized. The polarization resistance method was used to determine the uniform-corrosion rates of steel-3 and steel-35 in relation to the structure of fluorine-containing moieties of quaternary ammonium salts and their concentration

\\\\Expert2\\nbo\\Russian Journal of Applied Chemistry\\2011, v. 84, N 6, p.972.pdf
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8.
Инвентарный номер: нет.
   
   N 10


   
    N-(2-(2-Pyridyl)ethyl)chitosan (PEC) for Pd(II) and Pt(IV) sorption from HCl solutions [Text] / L. A. Santos Sorena, M. Ruiz, A. V. Pestov, A. M. Sastre, Yu. G. Yatluk, E. Guibal // Cellulose. - 2011. - Vol. 18, № 2. - P309-325. - Bibliogr. : p. 324-325 (32 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Chitosan was modified by grafting 2-pyridyl-ethyl moieties on the biopolymer backbone for the synthesis of a Platinum Group Metal (PGM) sorbent. The sorbent was tested for Pd(II) and Pt(IV) sorption from HCl solutions. Stable for HCl concentrations below 0.5 M, the sorbent reached sorption capacities as high as 3.2 and 2.6 mmol metal g?1 for Pd(II) and Pt(IV), respectively. Metal sorption mainly proceeds by electrostatic attraction in acidic solutions, though a contribution of complexation mechanism cannot be totally rejected. The resistance to intraparticle diffusion is the main controlling mechanism for uptake kinetics. While agitation speed has a limited effect on kinetics, metal concentration and sorbent dosage have a greater effect on the kinetic profiles. The intraparticle diffusivity varies between 3 ? 10?11 and 4.5 ? 10?10 m2 min?1. Thiourea (combined with HCl solution) is used for Pd(II) and Pt(IV) desorption. The resin could be desorbed and recycled for a minimum of five cycles maintaining high efficiencies of sorption and desorption

\\\\Expert2\\nbo\\Cellulose\\2011, v.18, p. 309.pdf
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9.
Инвентарный номер: нет.
   
   N 10


   
    N-(2-(2-Pyridyl)ethyl)chitosan (PEC) for Pd(II) and Pt(IV) sorption from HCl solutions [] / L. A. Santos Sorena, M. Ruiz, A. V. Pestov, A. M. Sastre, Yu. G. Yatluk, E. Guibal // Cellulose. - 2010. - 6 December. - Online first : рис., табл.
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Chitosan was modified by grafting 2-pyridyl-ethyl moieties on the biopolymer backbone for the synthesis of a Platinum Group Metal (PGM) sorbent. The sorbent was tested for Pd(II) and Pt(IV) sorption from HCl solutions. Stable for HCl concentrations below 0.5 M, the sorbent reached sorption capacities as high as 3.2 and 2.6 mmol metal g1 for Pd(II) and Pt(IV), respectively. Metal sorption mainly proceeds by electrostatic attraction in acidic solutions, though a contribution of complexation mechanism cannot be totally rejected. The resistance to intraparticle diffusion is the main controlling mechanism for uptake kinetics. While agitation speed has a limited effect on kinetics, metal concentration and sorbent dosage have a greater effect on the kinetic profiles. The intraparticle diffusivity varies between 3 10?11 and 4.5 1010 m2 min1. Thiourea (combined with HCl solution) is used for Pd(II) and Pt(IV) desorption. The resin could be desorbed and recycled for a minimum of five cycles maintaining high efficiencies of sorption and desorption

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10.
Инвентарный номер: нет.
   
   P 17


   
    Palladium and platinum sorption on a thiocarbamoyl-derivative of chitosan [Text] / A. Butewicz, K. Campos Galivan, A. V. Pestov, Yu. G. Yatluk, A. W. Trochimczuk, E. Guibal // Journal of Applied Polymer Science . - 2010. - Vol. 116, № 6. - P3318-3330 : рис.
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Immobilizing thiourea onto chitosan allowed using the polymer for the recovery of platinum groups metals (PGMs) in acidic solutions (up to 1–2M HCl concentrations). At low HCl concentration protonated amine groups may sorb chloroanionic metal species (electrostatic attraction mechanism); however, most of sorption proceeds through chelation on sulfur containing groups (less sensitive to acidic conditions). The bi-site Langmuir equation was used for fitting sorption isotherms. The sorption of PGMs was weakly affected by the composition of the solution (presence of high concentration of anions and base metals). Maximum sorption capacities for Pd(II) and Pt(IV) ranged between 274 and 330 mg g?1 in 0.25M HCl solutions and decreased to 150–198 mg g?1 in 2M HCl solutions: Pd(II) sorption was systematically higher than Pt(IV) sorption. The pseudo-second rate equation was used for modeling the uptake kinetics. Agitation speed hardly affected uptake kinetics indicating that external diffusion resistance is not the rate controlling step. Desorption yield higher than 85% were obtained using thiourea in 0.1M HCl solution. The adsorbents could be reused for at least three cycles

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