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 Найдено в других БД:Каталог книг и продолжающихся изданий (2)Публикации Чарушина В.Н. (9)Каталог библиотеки ИЭРиЖ УрО РАН (2)
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Общее количество найденных документов : 18
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 1-10    11-18 
1.
Инвентарный номер: нет.
   
   S 98

   
    Synthesis of new efficient and selective carboxylesterase inhibitors based on adamantyl and citronellyl 4,4,4-trifluoro-2-arylhydrazonylidene-3-oxobutanoates / N. A. Elkina, E. V. Shchegolkov, Ya. V. Burgart [et al.] // Russian chemical bulletin. - 2021. - Vol. 70, № 3. - P567–572
ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
4,4,4-TRIFLUORO-2-ARYLHYDRAZINYLIDENE-3-OXOBUTANOATES -- NATURAL ALCOHOLS -- CARBOXYLESTERASE -- INHIBITORS -- MOLECULAR DOCKING
Аннотация: A series of new adamantyl and citronellyl 4,4,4-trifluoro-2-arylhydrazinylidene-3-oxo-butanoates was synthesized. The synthesized compounds in nanomolar concentrations selectively inhibit carboxylesterase, while their activity is independent of the nature and position of the substituent in the aryl fragment, which is consistent with the molecular docking results.

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2.
Инвентарный номер: нет.
   
   S 98

   
    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 / V. L. Rusinov, I. M. Sapozhnikova, A. M. Bliznik, O. N. Chupakhin, V. N. Charushin, A. A. Spasov, P. M. Vassiliev, V. A. Kuznetsova, A. I. Rashchenko, D. A. Babkov // Archiv der Pharmazie. - 2017. - Vol. 350, № 5. - Pe1600361-[1]-e1600361-[15]
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
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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3.
Инвентарный номер: нет.
   
   S 98

   
    Synthesis and antitumour activity of 4-aminoquinazoline derivatives [Electronic resource] / G. N. Lipunova, E. V. Nosova, V. N. Charushin, O. N. Chupakhin // Russian Chemical Reviews. - 2016. - Vol. 85, № 7. - С. 759-793
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
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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4.
Инвентарный номер: нет.
   

   
    Polyfluoroalkyl-2-hydroxyimino-1,3-diketones as new selective carboxylesterase inhibitors / N. P. Boltneva, S. V. Lushchekina, O. G. Serebryakova [и др.] // MedChem-Russia 2021: материалы 5-ой Российской конференции по медицинской химии с международным участием. - Волгоград, 2021. - С. 256
Рубрики: ХИМИЧЕСКИЕ НАУКИ

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5.
Инвентарный номер: нет.
   

   
    Multitarget agents for the treatment of alzheimer's disease based on cholinesterase inhibitors / G. F. Makhaeva, N. V. Kovaleva, S. V. Lushchekina [и др.] // MedChem-Russia 2021: материалы 5-ой Российской конференции по медицинской химии с международным участием. - Волгоград, 2021. - С. 59
Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ
Кл.слова (ненормированные):
INHIBITORS CHOLINESTERASE

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6.
Инвентарный номер: нет.
   
   F 70

   
    Fluorinated derivatives of benz[4,5]imidazo[2,1-b][1,3]thiazoles are inhibitors of measles viruses [Электронный ресурс] / A. G. Pokrovskii, E. A. Il"ichyova, S. K. Kotovskaya, S. A. Romanova, V. N. Charushin, O. N. Chupakhin // Doklady Akademii Nauk . - 2004. - Vol.398, №3. - P412-414
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
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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7.
Инвентарный номер: нет.
   
   F 70

   
    Fluorinated derivatives of Benz[4,5]imidazo[1,2-b][1,3] thiazole - Inhibitors of reproduction of measles virus [Электронный ресурс] / A. G. Pokrovskii, E. A. Il"ichyova, S. K. Kotovskaya, S. A. Romanova, V. N. Charushin, O. N. Chupakhin // Doklady Biochemistry and Biophysics . - 2004. - Vol.398, №1-6. - P285-287
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
RIBAVIRIN -- ANTIVIRAL AGENTS -- THIAZOLES

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8.
Инвентарный номер: нет.
   
   D 62

   
    Direct Modification of Quercetin by 6-Nitroazolo[1,5-a]Pyrimidines [Electronic resource] / E. B. Gorbunov, G. L. Rusinov, E. N. Ulomskii, O. S. Eltsov, V. L. Rusinov, V. G. Kartsev, V. N. Charushin, I. A. Khalymbadzha, O. N. Chupakhin // Chemistry of Natural Compounds. - 2016. - Vol. 52, № 4. - С. 708-710
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
DERIVATIVES -- INHIBITORS -- ANALOGS

\\\\expert2\\NBO\\Chemistry of Heterocyclic Compounds\\2016, v.52, N 4, p. 708-710.pdf
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9.
Инвентарный номер: нет.
   
   D 46

   
    Design and Synthesis of N-Sulfonylamidines of Modafinic Acid [Electronic resource] / T. Beryozkina, V. A. Bakulev, L. Dianova, P. A. Slepukhin // Synthesis-Stuttgart. - 2016. - Vol. 48, № 7. - С. 1046-1054
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
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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10.
Инвентарный номер: нет.
   
   D 46

   
    Design and antioxidant properties of bifunctional 2H-imidazole-derived phenolic compounds-a new family of effective inhibitors for oxidative stress-associated destructive processes / E. L. Gerasimova, E. R. Gazizullina, M. V. Borisova [et al.] // Molecules. - 2021. - Vol. 26, № 21. - Ст. 6534
ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
2H-IMIDAZOLE -- POLYPHENOLS -- ANTIOXIDANT CAPACITY -- ANTIRADICAL CAPACITY
Аннотация: The synthesis of inhibitors for oxidative stress-associated destructive processes based on 2H-imidazole-derived phenolic compounds affording the bifunctional 2H-imidazole-derived phenolic compounds in good-to-excellent yields was reported. In particular, a series of bifunctional organic molecules of the 5-aryl-2H-imidazole family of various architectures bearing both electron-donating and electron-withdrawing substituents in the aryl fragment along with the different arrangements of the hydroxy groups in the polyphenol moiety, namely derivatives of phloroglucinol, pyrogallol, hydroxyquinol, including previously unknown water-soluble molecules, were studied. The structural and antioxidant properties of these bifunctional 5-aryl-2H-imidazoles were comprehensively studied. The redox transformations of the synthesized compounds were carried out. The integrated approach based on single and mixed mechanisms of antioxidant action, namely the AOC, ARC, Folin, and DPPH assays, were applied to estimate antioxidant activities. The relationship “structure-antioxidant properties” was established for each of the antioxidant action mechanisms. The conjugation effect was shown to result in a decrease in the mobility of the hydrogen atom, thus complicating the process of electron transfer in nearly all cases. On the contrary, the conjugation in imidazolyl substituted phloroglucinols was found to enhance their activity through the hydrogen transfer mechanism. Imidazole-derived polyphenolic compounds bearing the most electron-withdrawing functionality, namely the nitro group, were established to possess the higher values for both antioxidant and antiradical capacities. It was demonstrated that in the case of phloroglucinol derivatives, the conjugation effect resulted in a significant increase in the antiradical capacity (ARC) for a whole family of the considered 2H-imidazole-derived phenolic compounds in comparison with the corresponding unsubstituted phenols. Particularly, conjugation of the polyphenolic subunit with 2,2-dimethyl-5-(4-nitrophenyl)-2H-imidazol-4-yl fragment was shown to increase ARC from 2.26 to 5.16 (104 mol-eq/L). This means that the considered family of compounds is capable of exhibiting an antioxidant activity via transferring a hydrogen atom, exceeding the activity of known natural polyphenolic compounds.

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