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Общее количество найденных документов : 18
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 1-10    11-18 
1.

Вид документа : Статья из журнала
Шифр издания : 54
Автор(ы) : Deev S. L., Yasko M. V., Karpenko I. L., Ulomskii E. N., Chupakhin O. N.
Заглавие : 1,2,4-Triazoloazine derivatives as a new type of herpes simplex virus inhibitors
Место публикации : Bioorganic Chemistry . - 2010. - Vol. 38, № 6. - С. 265-270
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: A new class of inhibitors of herpes simplex virus replication was found. The compounds under study are derived from condensed 1,2,4-triazolo[5,1-c][1,2,4]triazines and 1,2,4-triazolo[1,5-a]pyrimidines, structural analogues of natural nucleic bases. Antiherpetic activity and cytotoxicity of the compounds were studied. The corresponding triphosphates of several active compounds were prepared and tested as inhibitors of DNA synthesis catalyzed by herpes simplex virus polymerase. The potential mechanism of their action is blocking of DNA dependent DNA polymerase, a key enzyme of viral replication
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2.

Вид документа : Статья из журнала
Шифр издания : 54/F 70
Автор(ы) : Pokrovskii A. G., Il"ichyova E.A., Kotovskaya S. K., Romanova S. A., Charushin V. N., Chupakhin O. N.
Заглавие : Fluorinated derivatives of benz[4,5]imidazo[2,1-b][1,3]thiazoles are inhibitors of measles viruses
Место публикации : Doklady Akademii Nauk . - 2004. - Vol.398, №3. - С. 412-414
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): antiviral activity--cytotoxicity--fluorinated benzimidazoles
Аннотация: The results of in vitro anti-virus activity investigation for the new benzimidazoles (their synthesis is reported previously) are presented. The activity of the most active compound was studied in dependence of its introduction to the culture (before virus adsorption, simultaneously with virus, directly after virus adsorption, after 6 hours and after 1 day). Preliminary treatment of cells didn't protect them from further infecting; therewith the compound introduction simultaneously with virus or after infection caused no considerable effect on its anti-virus activity. The latter is attributed to blocking of late stages of measles virus reproduction - synthesis or arrangement of virus proteins
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3.

Вид документа : Статья из журнала
Шифр издания : 54/F 70
Автор(ы) : Pokrovskii A. G., Il"ichyova E.A., Kotovskaya S. K., Romanova S. A., Charushin V. N., Chupakhin O. N.
Заглавие : Fluorinated derivatives of Benz[4,5]imidazo[1,2-b][1,3] thiazole - Inhibitors of reproduction of measles virus
Место публикации : Doklady Biochemistry and Biophysics . - 2004. - Vol.398, №1-6. - С. 285-287
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): ribavirin--antiviral agents--thiazoles
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4.

Вид документа : Статья из журнала
Шифр издания : 54/A 23
Автор(ы) : Utepova I. A., Trestsova M. A., Chupakhin O. N., Charushin V. N., Rempel A. A.
Заглавие : Aerobic oxidative C-H/C-H coupling of azaaromatics with indoles and pyrroles in the presence of TiO2 as a photocatalyst [Электронный ресурс]
Место публикации : Green Chemistry. - 2015. - Vol. 17, № 8. - С. 4401-4410
Систем. требования: http://apps.webofknowledge.com/
Примечания : Bibliogr. : p. 4409-4410 (30 ref.). - 18.01.2016
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): bond activation--inhibitors--hydrogen
Аннотация: In this paper we wish to report a highly selective and benign method for the double C-H/C-H coupling of azaaromatics with indoles or pyrrole in the presence of air oxygen/TiO2, as an effective photocatalytic oxidative system. It has been shown that this versatile approach can be applied for direct C-H functionalisation of a variety of azaaromatic systems, such as mono-, di- and triazines, substituted and unsubstituted azines and their benzo-annelated analogues.
\\\\expert2\\nbo\\Green Chemistry\\2015, v.17, N 8, p.4401-4410.pdf
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5.

Вид документа : Статья из журнала
Шифр издания : 54/A 37
Автор(ы) : Boltneva N. P., Makhaeva G. F., Kovaleva N. V., Lushchekina S. V., Burgart Ya. V., Shchegol’kov E. V., Chupakhin O. N.
Заглавие : Alkyl 2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates as new effective and selective inhibitors of carboxylesterase [Электронный ресурс]
Место публикации : Doklady Biochemistry and Biophysics . - 2015. - Vol. 465, № 1. - С. 381-385
Систем. требования: http://link.springer.com/article/10.1134/S1607672915060101
Примечания : Bibliogr. : p. 385 (15 ref.). - 19.01.2016
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): 2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates--inhibitors--carboxylesterase
Аннотация: A series of alkyl 2-Arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates was synthesized and their inhibitory activity with respect to porcine liver carboxylesterase (CaE, EC 3.1.1.1), human erythrocyte acetylcholinesterase (AChE, EC 3.1.1.7), and horse serum butyrylcholinesterase (BChE, EC 3.1.1.8) was studied. The molecular docking method was used to study the binding mode of the compounds in the active site of CaE. It was found that compounds containing the trifluoromethyl group in the third position of carbonyl chain are highly effective and selective inhibitors of CaE with nanomolar IC50 values, which agrees well with the results of molecular docking. Origin
\\\\expert2\\nbo\\Doklady Biochemistry and Biophysics\\2015, v.465, № 1. p.381-385.pdf
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6.

Вид документа : Статья из журнала
Шифр издания : 54/D 62
Автор(ы) : Gorbunov E. B., Rusinov G. L., Ulomskii E. N., Eltsov O. S., Rusinov V. L., Kartsev V. G., Charushin V. N., Khalymbadzha I. A., Chupakhin O. N.
Заглавие : Direct Modification of Quercetin by 6-Nitroazolo[1,5-a]Pyrimidines [Электронный ресурс]
Место публикации : Chemistry of Natural Compounds. - 2016. - Vol. 52, № 4. - С. 708-710
Систем. требования: http://apps.webofknowledge.com/
Примечания : 25.10.16
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): derivatives--inhibitors--analogs
\\\\expert2\\NBO\\Chemistry of Heterocyclic Compounds\\2016, v.52, N 4, p. 708-710.pdf
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7.

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Lipunova G. N., Nosova E. V., Charushin V. N., Chupakhin O. N.
Заглавие : Synthesis and antitumour activity of 4-aminoquinazoline derivatives [Электронный ресурс]
Место публикации : Russian Chemical Reviews. - 2016. - Vol. 85, № 7. - С. 759-793
Систем. требования: http://apps.webofknowledge.com/full
Примечания : 31.10.16
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): growth-factor receptor --potent egfr inhibitors--tyrosine kinase inhibitors
Аннотация: Scieces of data on the synthesis and antitumour activity of 4-aminoquinazolines are summarized and analyzed. Key methods for the synthesis of these compounds are considered, primarily cyclocondensation of carboxylic acid derivatives, as well as the oxidation of quinazolines and the cyclization of disubstituted thioureas. Improvements of synthetic schemes for erlotinib, gefitinib and lapatinib, which are the best-known pharmaceuticals based on compounds of the title class, are also considered. Synthetic strategies and biological activities for new 4-aminoquinazoline derivatives that are EGFR-tyrosine kinase inhibitors, multiactive compounds, and labelled compounds for use as positron emission tomography (PET) imaging agents are discussed.
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8.

Вид документа : Статья из журнала
Шифр издания : 54/D 46
Автор(ы) : Beryozkina T., Bakulev V. A., Dianova L., Slepukhin P. A.
Заглавие : Design and Synthesis of N-Sulfonylamidines of Modafinic Acid [Электронный ресурс]
Место публикации : Synthesis-Stuttgart. - 2016. - Vol. 48, № 7. - С. 1046-1054
Систем. требования: http://apps.webofknowledge.com/full
Примечания : 03.11.16
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): modafinil --n-sulfonyl amidines--dat inhibitors
Аннотация: A design and a convenient approach for the synthesis of novel N-sulfonyl-2-diphenylmethylsulfinylacetamidines have been demonstrated by starting from benzhydrylsulfanylacetic (BSA) acid. This approach involves a sequential amidation with amines, thionation with Lawesson's reagent, iminosulfonylation with sulfonyl azides, and oxidation of sulfide fragment with hydrogen peroxide. The key step of this transformation (reaction of thioamides with sulfonyl azides) was carried out either in ethanol or in the absence of any solvent. The synthesized compounds were tested in cells for inhibition of dopamine transporter. Among the synthesized compounds, two products were found to be in a similar range of activity as the well-known dopamine transporter inhibitor, modafinil.
\\\\expert2\\NBO\\Synthesis-Stuttgart\\2016. 48(7). 1046-1054.pdf
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9.

Вид документа : Статья из журнала
Шифр издания : 54/C 51
Автор(ы) : Kharitonova M. I., Antonov K. V., Fateev I. V., Berzina M. Ya., Kotovskaya S. K., Charushin V. N.
Заглавие : Chemoenzymatic Synthesis of Modified 2′-Deoxy-2′-fluoro-β-d-arabinofuranosyl Benzimidazoles and Evaluation of Their Activity Against Herpes Simplex Virus Type 1
Место публикации : Synthesis (Germany). - 2017. - Vol. 49, № 5. - С. 1043-1052
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): chemoenzymatic synthesis--benzimidazoles--herpes simplex virus type 1
Аннотация: 1-(2′-Deoxy-2′-fluoro-β-d-arabinofuranosyl)benzimidazoles containing 4,6-difluoro-, 4,5,6-trifluoro-, 5-fluoro-6-methoxy-, and 5-methoxy-4,6-difluorobenzimidazole fragments were synthesized by using purine nucleoside phosphorylase-catalyzed chemoenzymatic approach. As expected, enzymatic synthesis of nucleosides proceeds in lower yields of target compounds in comparison with the synthesis of ribo- and 2′-deoxyribobenzimidazoles (40–55% vs 60–90%). The compounds obtained were tested against the herpes simplex virus type 1, by using the Vero E6 cells. 5-Methoxy-4,6-difluoro-1-β-d-(2′-deoxy-2′-fluoroarabinofuranosyl)benzimidazole did not show any antiviral activity, when used in nontoxic concentration. All other nucleosides proved to exhibit a selective antiherpes activity. In contrast, it was shown that benzimidazole-β-d-arabinofuranosides of both di- and trisubstituted derivatives, having substituents in positions 4–6 of the benzene ring, as well as unsubstituted compounds, cannot be synthesized by enzymatic transglycosylation. 1-(β-d-Arabinofuranosyl)benzimidazole was obtained through glycosylation of N-trimethylsilylbenzimidazole with 1-chloro-2,3,5-O-methoxymethyl-d-arabinose. The behavior of this compound, as inhibitor of purine nucleoside phosphorylase (PNP) E. сoli, was investigated. 1-(β-d-Arabinofuranosyl)benzimidazole was found to belong to a mixed type of inhibitors of PNP. This fact explains why all attempts to perform enzymatic arabinosylation of 4,6-di-, 5,6-di-, and 4,5,6-trisubstituted benzimidazoles failed
\\\\expert2\\NBO\\Synthesis\\2017, v. 49(5), p. 1043-1052.pdf
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10.

Вид документа : Статья из журнала
Шифр издания : 54/S 98
Автор(ы) : Rusinov V. L., Sapozhnikova I. M., Bliznik A. M., Chupakhin O. N., Charushin V. N., Spasov A. A., Vassiliev P. M., Kuznetsova V. A., Rashchenko A. I., Babkov D. A.
Заглавие : Synthesis and Evaluation of Novel [1,2,4]Triazolo[5,1-c][1,2,4]-triazines and Pyrazolo[5,1-c][1,2,4]triazines as Potential Antidiabetic Agents
Место публикации : Archiv der Pharmazie. - 2017. - Vol. 350, № 5. - С. e1600361-[1]-e1600361-[15]
ББК : 54
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): antidiabetic agents--antiglycation -- azolotriazines --cross-link breakers--diabetes mellitus--dipeptidyl peptidase-4 inhibitors
Аннотация: Inhibition of the dipeptidyl peptidase-4 (DPP4) enzyme activity and prevention of advanced glycation end (AGE) products formation represents a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In the frames of this research study, several triazolo- and pyrazolotriazines were synthesized and evaluated as inhibitors of AGE products formation, DPP4, glycogen phosphorylase and α-glucosidase activities, as well as AGE cross-link breakers. From the two considered classes of heterocyclic compounds, the pyrazolotriazines showed the highest potency as antiglycating agents and DPP4 inhibitors. Structure–activity relationships (SAR) for these compounds, which can be considered as potential drugs for the treatment of type 2 diabetes, were evaluated.
\\\\Expert2\\NBO\\Archiv der Pharmazie\\2017 V 350 P.pdf
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