Центральная Научная Библиотека УрО РАН

Вид документа : Статья из журнала
Шифр издания : 54/D 55
Автор(ы) : Kataev V. E., Militsina O. I., Strobykina I. Yu., Gubaidullin A. T., Zverev V. V., Kataeva O. N., Fedorova O. V., Valova M. S., Rusinov G. L.
Заглавие : Diesters on the basis of 16-hydroxyisosteviol and dicarboxylic acids as carriers of Fe(III) picrates
Место публикации : Journal of Inclusion Phenomena and Macrocyclic Chemistry. - 2008. - Vol. 60, № 1-2. - С. 51-58
Примечания : Библиогр. : с. 58 (32 назв.)
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Diesters on the basis of 16-hydroxyisosteviol and dicarboxylic acids, exhibiting anti-tubercular activity, transport Fe(III) through liquid chloroform membrane which models a cell membrane. It is revealed that fluxes and anti-tubercular activity increase, as the length of the chain (spacer) between two ent-beyran skeletons of diesters increases. Computations on the level DFT/PBE explain the dependence of complexes stability on a structure of diterpenoid ligands. The structures of three diesters were established by single crystal X-ray analysis. ??
\\\\Expert2\\nbo\\Journal of Inclusion Phenomena and Macrocyclic Chemistry\\2008, V.60, N1-2, 51.pdf
Найти похожие

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Kotovskaya S. K., Zhumabaeva G. A., Perova N. M., Baskakova Z. M., Charushin V. N., Chupakhin O. N., Belanov E. F., Bormotov N. I., Balakhnin S. M., Serova O. A.
Заглавие : Synthesis and antiviral activity of fluorinated 3-phenyl-1,2,4-benzotriazines [Electronic resource]
Место публикации : Pharmaceutical Chemistry Journal. - 2007. - Vol. 41, № 2. - С. 62-68
Систем. требования: http://www.springerlink.com/content/b1m825j2867w2x00/fulltext.pdf
Примечания : Библиогр. : с. 68 (18 назв.). - 1.11.2011 г.
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: New synthetic approaches to fluorinated 3-phenyl-1,2,4-benzotriazines for biological testing have been elaborated. 1-(3,4-Difluorophenyl)-3,5-diphenylformazan (IVa) was synthesized via dinitriding of 3,4-difluoroaniline, followed by azo-addition of the resulting azobenzenediazonium chloride with acetaldehyde phenylhydrazone. 6,7-Difluoro-3-phenyl-1,2,4-benzotriazine (Va) was obtained via intramolecular cyclization of formazan IVa in the presence of BF3/AcOH complex. Monofluoro-substituted 6-R-7-fluoro-3-phenyl-1,2,4-benzotriazine derivatives (Vb-Vq) were prepared by substituting fluorine atom with alkoxides in 3,4-difluoronitrobenzene. Conditions for nucleophilic substitution of the second fluorine atom in benzotriazines V have been established. Fluorinated 3-phenyl-1,2,4-benzotriazines have been tested for antiviral and cytotoxic activity on Vero cell cultures and proved to be active against severe diseases caused by smallpox and some other pathogenic viruses. ??
\\\\Expert2\\nbo\\Pharmaceutical Chemistry Journal\\2007, 41 (2), 62.pdf
Найти похожие

Вид документа : Статья из журнала
Шифр издания : 54/T 44
Автор(ы) : Rusinov V. L.
Заглавие : The scintillator tile hadronic calorimeter prototype
Место публикации : Nuclear Physics B, Proceedings Supplements. - 2006. - Vol. 150: Innovative Particle and Radiation Detectors. - С. 253-256
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: A high granularity scintillator hadronic calorimeter prototype is described. The calorimeter is based on a novel photodetector - Silicon Photo-Multiplier (SiPM). The main parameters of SiPM are discussed as well as readout cell construction and optimization. The experience with a small prototype production and testing is described. A new 8 k channel prototype is being manufactured now.
Найти похожие

Вид документа : Статья из журнала
Шифр издания : 54/T 44
Автор(ы) : Medvedeva N., Polyak Yu., Kuzikova I., Orlova O., Zharikov G.
Заглавие : The effect of mustard gas on the biological activity of soil
Место публикации : Environmental Research. - 2008. - Vol. 106, № 3. - С. 289-295
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: A special group of substances that are very dangerous for the biosphere includes war gases such as mustard gas (bis(2-chloroethyl)sulphide). The influence of mustard gas hydrolysis products (MGHPs) on soil microbiota has been investigated. These substances bear numerous toxic effects on soil microorganisms. They change significantly the number and the specific composition of soil microbiota and inhibit the enzyme activity of soils. The main "ecological targets" of mustard and its hydrolysis products' toxic action have been determined. MGHPs affect the growth and reproduction of soil micromycetes, as well as their morphological and cultural properties. Increase in number and size of mitochondria in the fungal cells is accompanied by increase in dehydrogenases activity. Cell permeability influenced by MGHPs grows in connection with concentration of toxicants. Increase of permeability corresponds to growth of the amount of unsaturated fatty acids. The changes in the fatty acid composition of lipids in the cells of the soil micromycetes display their adaptation to adverse impact of the substances studied. MGHPs and thiodiglycol enhance synthesis of polysaccharides and pigments.
Найти похожие

Вид документа : Статья из журнала
Шифр издания : 54/H 86
Автор(ы) : Hristov P.K., Petrov L.A., Russanov E.M.
Заглавие : Lipid peroxidation induced by ultrasonication in Ehrlich ascitic tumor cells
Место публикации : Cancer Letters. - 1997. - Vol.121, N1. - С. 7-10
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The mechanism of sonodynamic action in tumor cells is poorly investigated. It is known that ultrasound generates free radicals in phosphatidylcholine liposomes used as a membrane model. The participation of lipid peroxidation products in the mechanisms of physiological suppression of cell multiplication has been investigated for some tumor cells
Найти похожие

Вид документа : Статья из журнала
Шифр издания : 54/C 74
Автор(ы) : Skorik Yu. A., Gomes C. A. R. , Podberezskaya N. V. , Romanenko G. V., Pinto L. F., Yatluk Yu. G.
Заглавие : Complexation models of N-(2-carboxyethyl)chitosans with copper(II) ions
Место публикации : Biomacromolecules. - 2005. - Vol. 6, № 1. - С. 189-195. - ISSN 1525-7797. - ISSN 1525-7797
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The copper(II) complex formation equilibria of N-(2-carboxyethyl)chitosans with three different degrees of substitution (DS = 0.42, 0.92, and 1.61) were studied in aqueous solution by pH-potentiometric and UV-spectrophotometric techniques. It was demonstrated that the complexation model of CE-chitosans depends on DS: the [Cu(Glc-NR2)2] complexes are predominant for two lower substituted samples ("bridge model", log ?12 = 10.06 and 11.6, respectively), whereas the increase of DS leads to formation mainly of the [Cu(Glc-NR2)] complexes ("pendant model", log ?11 = 6.41). As a model for copper complexation with a disubstituted residue of CE-chitosan, the complex of N-methyliminodipropionate [CuMidp(H2O)]·(H2O) was synthesized and structurally characterized by XRD. The unit cell consists of two crystallographically nonequivalent Cu atoms having slightly distorted square pyramidal coordination; Midp constitutes the basal plane of the pyramid and acts as a tetradentate NO3 chelate-bridging ligand by the formation of two six-membered chelate rings (average Cu-O 1.99 A, Cu-N 2.04 A) and a bridge via carbonyl O atom (average Cu-O 1.99 A), an apical position is occupied by a water molecule (average Cu-Ow 2.30 A).
Найти похожие

Вид документа : Статья из журнала
Шифр издания : 54/C 51
Автор(ы) : Bushkova O. V., Andreev O. L., Batalov N. N., Shkerin S. N., Kuznetsov M. V., Koryakova O. V., Song E. N., Chung H. J.
Заглавие : Chemical interactions in the cathode half-cell of lithium-ion batteries: Part I. Thermodynamic simulation
Место публикации : Journal of Power Sources. - 2006. - Vol. 157, № 1. - С. 477-482
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The method of thermodynamic simulation was used to study chemical interactions in the cathode half-cell of lithium-ion battery, which contained LiCoO2 as cathode active material and a LiPF6 solution as the electrolyte. It was shown that in the temperature range 298–400 K in thermodynamic equilibrium state a layer of solid products of chemical reaction formed on the cathode/electrolyte interface. The layer predominantly consisted of LiF and LiPO3 in the molar ratio about 2:1 (corresponding to the volume ratio 2:3). In equilibrium state also some soluble interaction products formed, namely: CoF2 (considerable quantity), POF3 and PF5. The concentration of the later two substances was small, but it increased with increase of the temperature. Furthermore, in equilibrium state oxygen gas formed as a product of chemical interactions in cathode half-cell.????Thermodynamic characteristics of Co2O3 and LiCoO2 compounds were determined using a set of calculation methods??
Найти похожие

Вид документа : Статья из журнала
Шифр издания : 54/A 62
Автор(ы) : Kogan G., Skorik Yu.A., Zitnanova I., Krizkova L., Durackova Z., Gomes C. A. R., Yatluk Yu. G., Krajcovic J.
Заглавие : Antioxidant and antimutagenic activity of N-(2-carboxyethyl)chitosan
Место публикации : Toxicology and Applied Pharmacology . - 2004. - Vol. 201, № 3. - С. 303-310: ил.
Примечания : Библиогр.: с. 309-310 (49 ref.)
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The antioxidant and antimutagenic activities of the novel carboxyethyl derivatives of chitosan with three different degrees of substitution have been assayed in vitro in the unicellular flagellate Euglena gracilis subjected to the action of genotoxic agents acridine orange and ofloxacin. It has been demonstrated that chitosan derivatives exhibit concentration-dependent protective antigenotoxic activity against both mutagens. It is suggested that different mechanisms may be involved in its protective action—antioxidant activity in case of ofloxacin-induced DNA damage, as well as possible interaction with the cell membrane that prevents acridine orange from reaching the genetic compartments and subsequent damaging DNA through intercalative binding. Direct adsorption of acridine orange on chitosan derivatives was ruled out as a possible mechanism of protection on the basis of spectrophotometric measurements. Dependence of the antimutagenic properties of the studied chitosan derivatives on the degree of substitution was reversed in experiments involving acridine orange and ofloxacin, which also indicated different mechanisms of protection involved in these two cases.????
Найти похожие

Вид документа : Статья из журнала
Шифр издания : 54/A 62
Автор(ы) : Karpenko I. L., Deev S. L., Kiselev O. I., Charushin V. N., Rusinov V. L., Ulomskii E. N., Deeva E.G., Chupakhin O. N.
Заглавие : Antiviral Properties, Metabolism, and Pharmacokinetics of a Novel Azolo-1,2,4-Triazine-Derived Inhibitor of Influenza A and B Virus Replication
Место публикации : Antimicrobial Agents and Chemotherapy. - 2010. - Vol. 54, № 5. - С. 2017-2022
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Influenza viruses of types A and B cause periodic pandemics in the human population. The antiviral drugs approved to combat influenza virus infections are currently limited. We have investigated an effective novel inhibitor of human influenza A and B viruses, triazavirine {2-methylthio-6-nitro-1,2,4-triazolo[5,1-c]-1,2,4-triazine-7(4I)-one} (TZV). TZV suppressed the replication of influenza virus in cell culture and in chicken chorioallantoic membranes, and it protected mice from death caused by type A and B influenza viruses. TZV was also effective against a rimantadine-resistant influenza virus strain and against avian influenza A virus H5N1 strains. The pharmacokinetic parameters and bioavailability of TZV were calculated after the administration of TZV to rabbits. The TZV metabolite AMTZV {2-methylthio-6-amino-1,2,4-triazolo[5,1-s]-1,2,4-triazin(e)-7(4I)-one} was discovered in IAK 293T and Huh7 cell cultures, a liver homogenate, and rabbit blood after intragastric administration of TZV. AMTZV was nontoxic and inactive as an inhibitor of influenza virus in cell culture. Most likely, this metabolite is a product of TZV elimination
Найти похожие

10.

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Egorov I. N., Rusinov V. L., Slepukhin P. A., Chupakhin O. N.
Заглавие : Synthesis and Crystal Structure of (S)-2-((S)-2-(N-Ts-Amino)-3-methylbutanoyl)-3-(1H-indol-3-yl)-6-phenyl-3,4-dihydro-1,2,4-triazin-5(2H)-one [Electronic resource]
Место публикации : Journal of Chemical Crystallography . - 2010. - Vol. 40, № 4. - С. 387-390
Систем. требования: http://www.springerlink.com/content/h067587131031v7t/fulltext.pdf
Примечания : 2.11.2011 г.
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The diastereoselective synthesis, NMR and X-ray structure of (S)-2-((S)-2-(N-Ts-amino)-3-methylbutanoyl)-3-(1H-indol-3-yl)-6-phenyl-3,4-dihydro-1,2,4-triazin-5(2H)-one—a potential antivirus agent are reported. The compound crystallizes in the triclinic space group P1 with unit cell parameters: a = 5.9259(6) A, b = 9.6370(12) A, c = 12.9541(9) A, = 109.210(9)°, beta = 90.804(7)°, y = 105.074(10)° and Z = 1.
\\\\Expert2\\nbo\\Journal of Chemical Crystallography\\2010.v.40, N 4, p.387.pdf
Найти похожие

11.

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Lipunova G. N., Nosova E. V., Sidorova L. P., Charushin V. N.
Заглавие : Synthesis and antitumor activity of fluorinated derivatives of [i,j]-annelated quinolones [Electronic resource]
Место публикации : Pharmaceutical Chemistry Journal. - 2011. - Vol. 45, № 4. - С. 208-210: ил.
Систем. требования: http://www.springerlink.com/content/4x40438141525728/fulltext.pdf
Примечания : Bibliogr. : p. 210 (7 ref.). - 1.11.2011 г.
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Tri- and pentacyclic fluoroquinolones were synthesized by intramolecular cyclization of the corresponding 3-hydrazinopolyfluorobenzoylacrylates followed by substitution of fluorine atoms by amine residues. The antitumor activity of the resulting compounds was studied at the National Cancer Institute using cultures of 60 cell lines of nine groups, including leukemia, lung tumor, large intestine tumor, CNS tumor, melanoma, ovary tumor, renal tumor, prostate tumor, and breast tumor. Relationships between structure and antitumor activity were analyzed. In vivo experimental data from hollow fiber tests are presented for two derivatives
\\\\Expert2\\nbo\\Pharmaceutical Chemistry Journal\\2011, 45 (4), 208.pdf
Найти похожие

12.

Вид документа : Статья из журнала
Шифр издания : 54/T 80
Автор(ы) : Loginova S. A., Borisevich S. V., Rusinov V. L., Ulomskii E. N., Charushin V. N., Chupakhin O. N.
Заглавие : Toxicity of Triazavirin, a Novel Russian Antiinfluenza chemotherapeutic
Место публикации : Antibiotiki i Khimioterapiya . - 2012. - Vol.57, №11-12. - 8-10
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): mice--toxicity--triazavirin
Аннотация: The study of the toxicity of triazavirin, a new antiinfluenza agent, showed that the maximum concentration of the drug, inducing no microscopically visible changes in the structure of the monolayer and the cells of the MDCK and SKEV cell cultures, was 128 and 100 mcg/ml respectively. The maximum drug dose for single intraperitoneal administration inducing no signs of acute intoxication in albino mice weighing 10-12 g was 1000 mg/kg. In investigation of the chronic toxicity it was shown that oral administration of the drug (by 0.05 ml) to the albino mice in a dose of 200 mg/kg (maximum possible concentration by the solubility) daily for 10 days was well tolerated by the laboratory animals. The maximum tolerable dose of triazavirin for the albino mice was 200 mg/kg.
Найти похожие

13.

Вид документа : Статья из журнала
Шифр издания : 54/A 62
Автор(ы) : Karpenko I. L., Deev S. L., Kiselev O. I., Charushin V. N., Rusinov V. L., Ulomskii E. N., Deeva E.G., Kukhanova M. K.
Заглавие : Antiviral properties, metabolism, and pharmacokinetics of a novel azolo-1,2,4-triazine-derived inhibitor of influenza A and B virus replication
Место публикации : Antimicrobial Agents and Chemotherapy . - 2010. - Vol.54, №5. - С. 2017-2022
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): animal cell--animal experiment--antiviral activity
Аннотация: Influenza viruses of types A and B cause periodic pandemics in the human population. The antiviral drugs approved to combat influenza virus infections are currently limited. We have investigated an effective novel inhibitor of human influenza A and B viruses, triazavirine {2-methylthio-6-nitro-1,2,4- triazolo[5,1-c]-1,2,4-triazine-7(4Í)-one} (TZV). TZV suppressed the replication of influenza virus in cell culture and in chicken chorioallantoic membranes, and it protected mice from death caused by type A and B influenza viruses. TZV was also effective against a rimantadine-resistant influenza virus strain and against avian influenza A virus H5N1 strains. The pharmacokinetic parameters and bioavailability of TZV were calculated after the administration of TZV to rabbits. The TZV metabolite AMTZV {2-methylthio-6-amino-1,2,4- triazolo[5,1-s]-1,2,4-triazin(e)-7(4Í)-one} was discovered inÍÅK 293T and Huh7 cell cultures, a liver homogenate, and rabbit blood after intragastric administration of TZV. AMTZV was nontoxic and inactive as an inhibitor of influenza virus in cell culture. Most likely, this metabolite is a product of TZV elimination
Найти похожие

14.

Вид документа : Статья из журнала
Шифр издания : 54/I-70
Автор(ы) : Loginova S. Ya., Borisevich S. V., Maksimov V. A., Bondarev V. P., Kotovskaya S. K., Rusinov V. L., Charushin V. N.
Заглавие : Investigation of triazavirin antiviral activity against influenza A virus (H5N1) in cell culture
Место публикации : Antibiotiki i Khimioterapiya . - 2007. - Vol.52, №11-12. - С. 18-20
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): antiviral activity--arbidol--influenza
Аннотация: Analysis of triazavirin efficacy with respect to influenza A virus (H5N1) in sensitive cell culture MDSK vs. effective antigrippe drugs, such as tamiflu, remantadin and arbidol showed that triazavirin in a wide range of the concentrations was efficient in inhibition of the virus cytopathic activity and formation of the specific hemagglutinin
Найти похожие

15.

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Kotovskaya S. K., Zhumabaeva G. A., Perova N. M., Baskakova Z. M., Charushin V. N., Chupakhin O. N., Belanov E. F., Serova O. A.
Заглавие : Synthesis and antiviral activity of fluorinated 3-phenyl-1,2,4- benzotriazines
Место публикации : Pharmaceutical Chemistry Journal. - 2007. - Vol.41, №2. - С. 62-68
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): cyclization--cytotoxicity--fluorination
Аннотация: New synthetic approaches to fluorinated 3-phenyl-1,2,4-benzotriazines for biological testing have been elaborated. 1-(3,4-Difluorophenyl)-3,5- diphenylformazan (IVa) was synthesized via dinitriding of 3,4-difluoroaniline, followed by azo-addition of the resulting azobenzenediazonium chloride with acetaldehyde phenylhydrazone. 6,7-Difluoro-3-phenyl-1,2,4-benzotriazine (Va) was obtained via intramolecular cyclization of formazan IVa in the presence of BF3/AcOH complex. Monofluoro-substituted 6-R-7-fluoro-3-phenyl-1,2,4- benzotriazine derivatives (Vb-Vq) were prepared by substituting fluorine atom with alkoxides in 3,4-difluoronitrobenzene. Conditions for nucleophilic substitution of the second fluorine atom in benzotriazines V have been established. Fluorinated 3-phenyl-1,2,4-benzotriazines have been tested for antiviral and cytotoxic activity on Vero cell cultures and proved to be active against severe diseases caused by smallpox and some other pathogenic viruses
Найти похожие

16.

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Grishko V. V., Tolmacheva I. A., Galaiko N. V., Pereslavceva A. V., Anikina L. V., Volkova L. V., Bachmetyev B. A., Slepukhin P. A.
Заглавие : Synthesis, transformation and biological evaluation of 2,3-secotriterpene acetylhydrazones and their derivatives
Место публикации : European Journal of Medicinal Chemisrty. - 2013. - Vol.68. - С. 203-211
Примечания : Bibliogr. : p. 211 (34 ref.)
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): antiviral activity--acetylhydrazone--betulonic acid
Аннотация: It has been previously shown that semi-synthetic A-secotriterpene acetylhydrazones of 1-cyano-28-methoxy-28-oxo-2,3-seco-2-norlup-20(29)-en-3-al and 1-cyano-2,3-seco-2-nor-19β,28-epoxy-18αH-olean-3-al (1, 2) inhibit the vesicular stomatitis virus (VSV) replication. To improve the antiviral activity against VSV, structural modifications of compounds 1 and 2 were performed, and new A-secoderivatives containing the acetylhydrazone fragment were obtained from betulonic acid and its methyl ester, allobetulone, and 3-oxo-18βH-glycyrrhetinic acid methyl ester. The inhibitory effects of these compounds on VSV replication in porcine embryo kidney (PEK) cells were determined after infection. It was shown that introduction of the 3′-acetyl-5′-methyl-1′,3′,4′-oxadiazoline fragment into lupane triterpene structures lead to an increase in the antiviral activity of A-secotriterpene derivatives. However, the presence of a heterocyclic moiety enhanced toxic activity and reduced the therapeutic indices of these agents. Investigation in the anti-proliferative activity of the heterocyclic derivatives has shown high sensitivity of A-549, MS and RD tumor cell lines to lupane (R)-oxadiazoline 11a. The pro-apoptotic effect of 11a was confirmed by the AnnexinV/PI analysis
\\\\expert2\\NBO\\European Journal of Medicinal Chemistry\\2013, v.68, p.203.pdf
Найти похожие

17.

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Galaiko N. V., Nazarov A. V., Tolmacheva I. A., Slepukhin P. A., Vikharev Y. B., Maiorova O. A., Grishko V. V.
Заглавие : Synthesis of Triterpene A-Condensed Azoles
Место публикации : Chemistry of Heterocyclic Compounds. - 2014. - С. Article in Press
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): alfa-hydroximino ketones--1,2,3-triazoles--allobetulone
Аннотация: Lupane and 18αH-oleanane α-hydroximino ketones were used to synthesize derivatives condensed at ring A with a substituted azole fragment, namely, C(2)-C(3)-fused oxazoles and 1,2,3-triazoles. Triterpene isoxazoles fused at the C(1)-C(2) bond are described for the first time. An optimized method was proposed for the synthesis of unsubstituted 1,2,3-triazoles, displaying cytotoxic activity (IC50 8.4-40.7 μM) relative to rhabdomyosarcoma, lung carcinoma, and MS melanoma cell lines.
Найти похожие

18.

Вид документа : Статья из журнала
Шифр издания : 54/C 51
Автор(ы) : Kharitonova M. I., Fateev I. V., Kayushin A. L., Konstantinova I. D., Kotovskaya S. K., Andropova V. L., Galegov G. A., Charushin V. N., Miroshnikov A. I.
Заглавие : Chemoenzymatic Synthesis and Antiherpes Activity of 5-Substituted 4,6-Difluorobenzimidazoles Ribo- and 2′-Deoxyribonucleosides [Электронный ресурс]
Место публикации : Synthesis (Germany). - 2016. - Vol. 48, № 3. - С. 394-406
Систем. требования: https://www.thieme-connect.com/products/ejournals/html/10.1055/s-0035-1560911
Примечания : Bibliogr. : p. 405-406 (37 ref.). - 29.03.16
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): drug discovery---nucleosides--herpes simplex virus
Аннотация: A series of 5,6-disubstituted benzimidazole nucleosides, obtained earlier, did not show any significant antiviral activity at relatively low cytotoxicity in vitro. In the course of our research we have succeeded in introducing an additional fluorine atom into the benzimidazole ring system. A new series of 4,6-difluorobenzimidazoles, bearing various groups (fluoro-, methoxy-, ethoxy-, morpholino-, and pyrrolidino-) in the 5-position of the benzene ring, have been synthesized. All these compounds proved to be substrates for recombinant E. coli purine nucleoside phosphorylase (PNP) in the transglycosylation reaction. Effective methods for the synthesis of ribo- and 2′-deoxyribonucleosides with high yields (60–90%) have been described, and the formation of regioisomeric N3-nucleosides of benzimidazoles have been detected. The biological activity of the nucleosides obtained against herpes simplex virus type 1 (HSV-1) has been elucidated. All compounds show a low cytotoxicity in the cell culture Vero E6. 4,5,6-Trifluoro-1-(β-d-ribofuranosyl)benzimidazole and 5-methoxy-4,6-difluoro-1-(β-d-2′-deoxyribofuranosyl)benzimidazole proved to inhibit completely the progression of the virus cytopathic effect (CPE) at a multiplicity of infection (MOI) of 0.01 PFU/cell.
\\\\expert2\\nbo\\Synthesis\\2016, v. 48. p.394-406.pdf
Найти похожие

19.

Вид документа : Статья из журнала
Шифр издания : 54
Автор(ы) : Lipunova G. N., Nosova E. V., Charushin V. N., Chupakhin O. N.
Заглавие : Boron(III) Complexes with N,N'- and N,O-Heterocyclic Ligands: Synthesis and Spectroscopic Properties
Место публикации : Comments on Inorganic Chemistry. - 2016. - Vol. 2016. - С. 1153470
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): properties --preparation-- synthetic preparation
Аннотация: This review is focused on consideration of effects of the nature of N,N'- and N,O-bidentate ligands on the structure and optical properties of their B(III) complexes. It has been established that B(III) complexes with asym. N,N'- and N,O-bidentate ligands, such as ortho-hydroxyphenyl substituted azaheterocycles and heteryl-β-ketoimines, exhibit large Stokes shifts, enhanced intensity, and extended range for luminescence in solns. as well as in solid state, comparable with characteristics of the family of BODIPYs derivs. Complexes of some bidentate ligands can be considered as promising fluorophores for applications in biomedical imaging, electroluminescent, solar cell devices, and other fields.
\\\\expert2\\nbo\\Comments on Inorganic Chemistry\\2016. P. 1153470.pdf
Найти похожие

20.

Вид документа :
Шифр издания : 54/E 27
Автор(ы) : Shevelev O. B., Illarionova N. B., Petrovski D. V., Sarapultsev A. P., Chupakhin O. N., Moshkin M. P.
Заглавие : Effects of a compound from the group of substituted thiadiazines with hypothermia inducing properties on brain metabolism in rats, a study in vivo and in vitro
Место публикации : PLOS ONE . - 2017. - Vol. 12, № 7. - С. е0180739[1-12]
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): гипотермия--hypothermia--1,3,4-thiadiazine--метаболиты мозга--brain metabolites--терморегуляция--thermoregulation
Аннотация: The aim of the present study was to examine how administration of a compound of 1,3,4-thiadiazine class 2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide (L-17) with hypothermia inducing properties affects the brain metabolism. The mechanism by which L-17 induces hypothermia is unknown; it may involve hypothalamic central thermoregulation as well as act via inhibition of energy metabolism. We tested the hypothesis that L-17 may induce hypothermia by directly inhibiting energy metabolism. The study in vivo was carried out on Sprague-Dawley adult rats. Two doses of L-17 were administered (190 mg/ kg and 760 mg/kg). Brain metabolites were analyzed in control and treated groups using magnetic resonance spectroscopy, along with blood flow rate measurements in carotid arteries and body temperature measurements. Further in vitro studies on primary cultures from rat hippocampus were carried out to perform a mitochondria function test of L-17 preincubation (100 μM, 30 min). Analysis of brain metabolites showed no significant changes in 190 mg/kg treated group along with a significant reduction in body temperature by 1.5ÊC. However, administration of L-17 in higher dose 760 mg/kg provoked changes in brain metabolites indicative of neurotoxicity as well as reduction in carotid arteries flow rate. In addition, a balance change of excitatory and inhibitory neurotransmitters was observed. The L-17 pre-incubation with cell primary cultures from rat brain showed no significant changes in mitochondrial function. The results obtained in the study indicate that acute administration of L-17 190 mg/kg in rats induces mild hypothermia with no adverse effects onto brain metabolism.
\\\\Expert2\\NBO\\PLoS ONE\\2017 V. 12 N 7 p. e0180739.pdf
Найти похожие

1-20 21-33

Сиглы отделов ЦНБ УрО РАН

  бр.ф. - Бронированный фонд

  бф - Научно-библиографический отдел

  БХЛ - Фонд художественной литературы

  ИИиА -Фонд исторической литературы в ЦНБ УрО РАН

  ИМЕТ -Отдел ЦНБ в Институте металлургии УрО РАН

  кх - Отдел фондов (книгохранениe)

  МБА - Межбиблиотечный абонемент

  мф - Методический фонд

  ок - Отдел научной каталогизации

  оку - Отдел комплектования и учета

  орф - Обменно-резервный фонд

  пф - Читальный зал деловой и патентной информации

  рк - Фонд редкой книги

  ч/з - Главный читальный зал

  эр - Зал электронных ресурсов

Сиглы библиотек институтов и НЦ УрО РАН

© Международная Ассоциация пользователей и разработчиков электронных библиотек и новых информационных технологий
(Ассоциация ЭБНИТ)