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Общее количество найденных документов : 14
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 1-10    11-14 
1.
Инвентарный номер: нет.
   
   P 72


   
    Platelet aggregation inhibitor properties of 1,3,4-thiadiazine thiadiazines [Text] / T. M. Vasilyeva, V. A. Makarov, O. N. Chupakhin, L. P. Sidorova, N. M. Perova, V. L. Rusinov // Gematologiya i Transfusiologiya . - 2008. - Vol. 53, № 4. - P12-15. - Bibliogr. : p. 15 (14 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
1,3,4-THIADIAZINES -- PLATELET AGGREGATION -- ARACHIDONIC ACID -- ADP
Аннотация: Effects of new 1,3,4-thiadiazines on human platelet aggregation were studied in vitro. All 1,3,4-thiadiazines inhibited aggregation induced by ADP and arachidonic acid in a wide range of concentrations. The most active of the studied 1,3,4-thiadiazines were L-19, L-20, L-25, L-28, and L-31 in concentrations of 0.01-1 mM, effectively reducing platelet aggregation induced by arachidonic acid and ADP.

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2.
Инвентарный номер: нет.
   
   A 62


   
    Antiviral properties, metabolism, and pharmacokinetics of a novel azolo-1,2,4-triazine-derived inhibitor of influenza A and B virus replication [Электронный ресурс] / I. L. Karpenko, S. L. Deev, O. I. Kiselev, V. N. Charushin, V. L. Rusinov, E. N. Ulomskii, E. G. Deeva, M. K. Kukhanova // Antimicrobial Agents and Chemotherapy . - 2010. - Vol.54, №5. - P2017-2022
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
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

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3.
Инвентарный номер: нет.
   
   A 62


   
    Antiviral Properties, Metabolism, and Pharmacokinetics of a Novel Azolo-1,2,4-Triazine-Derived Inhibitor of Influenza A and B Virus Replication [Text] / I. L. Karpenko, S. L. Deev, O. I. Kiselev, V. N. Charushin, V. L. Rusinov, E. N. Ulomskii, E. G. Deeva, O. N. Chupakhin // Antimicrobial Agents and Chemotherapy. - 2010. - Vol. 54, № 5. - P2017-2022
ББК 54
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

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4.
Инвентарный номер: нет.
   
   F 97


   
    Functionalization, cyclization and antiviral activity of A-secotriterpenoids [Electronic resource] / V. V. Grishko, N. V. Galaiko, I. A. Tolmacheva, I. I. Kucherov, V. F. Eremin, E. I. Boreco, O. V. Savinova, P. A. Slepukhin // European Journal of Medicinal Chemisrty. - 2014. - Vol. 83. - С. 601-608
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
A-SECOTRITERPENOIDS -- BETULIN -- 18βH-GLYCYRRHETINIC ACID
Аннотация: Triterpene derivatives with an α,β-alkenenitrile moiety in the five-membered ring A have been synthesized by nitrile anion cyclizations of 1-cyano-2,3-secotriterpenoids. Oxime-containing precursors, 2,3-secointermediates and five-membered ring A products of cyclizations were screened for in vitro antiviral activity against enveloped viruses – influenza A virus and human immunodeficiency virus type I (HIV-1). Lupane ketoxime and the 2,3-secolupane C-3 aldoxime which possess antiviral activities against both influenza A virus (EC50 12.9–18.2 μM) and HIV-1 (EC50 0.06 μM) were the most promising compounds.

\\\\expert2\\nbo\\European Journal of Medicinal Chemistry\\2014, v.83, p.601-608.pdf
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5.
Инвентарный номер: нет.
   
   F 97


   
    Functionalization, cyclization and antiviral activity of A-secotriterpenoids / V. V. Grishko, N. V. Galaiko, I. A. Tolmacheva, O. V. Savinova, P. A. Slepukhin // European Journal of Medicinal Chemisrty. - 2014. - Vol.83. - С. 601-608. - Bibliogr. : p. 608 (37 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
18βH-GLYCYRRHETINIC ACID -- A-SECOTRITERPENOIDS -- ANTIVIRAL ACTIVITY
Аннотация: Triterpene derivatives with an α,β-alkenenitrile moiety in the five-membered ring A have been synthesized by nitrile anion cyclizations of 1-cyano-2,3-secotriterpenoids. Oxime-containing precursors, 2,3- secointermediates and five-membered ring A products of cyclizations were screened for in vitro antiviral activity against enveloped viruses - influenza A virus and human immunodeficiency virus type I (HIV-1). Lupane ketoxime and the 2,3-secolupane C-3 aldoxime which possess antiviral activities against both influenza A virus (EC50 12.9-18.2 μM) and HIV-1 (EC50 0.06 μM) were the most promising compounds.

\\\\expert2\\nbo\\European Journal of Medicinal Chemistry\\2014, v.83, p.601-608.pdf
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6.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis of A-Pentacyclic Triterpene α,β-Alkenenitriles [Electronic resource] / A. V. Pereslavceva, I. A. Tolmacheva, P. A. Slepukhin, O. S. Eltsov, I. I. Kucherov, V. F. Eremin, V. V. Grishko // Chemistry of Natural Compounds. - 2014. - Vol.49, №6. - С. 1059-1066. - Bibliogr. : p. 1066 (24 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ALFA,BETA- ALKENENITRILES -- A-SECO-TRITERPENOIDS -- ALLOBETULONE
Аннотация: A-seco-triterpenoids with a methylketone group were synthesized from epimeric 3-hydroxy-3-methyl-1-cyano-2,3-seco-triterpenoids of the lupane and 19β,28-epoxy-18αH-oleanane types, which were formed by a Grignard reaction. The resulting methylketones underwent under base-catalysis conditions an intramolecular cyclization to form A-pentacyclic β-substituted alkenenitriles. The synthesized compounds included 3-methyl-1-cyano-19β,28- epoxy-2,3-seco-2-nor-18αH-olean-3-one and methyl 3-methyl-1-cyano-2- norlup-1(3),20(29)-dien-28-oate, which inhibited in vitro reproduction of human immunodeficiency virus type 1.

\\\\expert2\\nbo\\Chemistry of Natural Compounds\\2014, V.49, N6, p.1059.pdf
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7.
Инвентарный номер: нет.
   
   A 37


   
    Alkyl 2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates as new effective and selective inhibitors of carboxylesterase [Electronic resource] / N. P. Boltneva, G. F. Makhaeva, N. V. Kovaleva, S. V. Lushchekina, Ya. V. Burgart, E. V. Shchegol’kov, O. N. Chupakhin // Doklady Biochemistry and Biophysics . - 2015. - Vol. 465, № 1. - С. 381-385. - Bibliogr. : p. 385 (15 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
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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8.
Инвентарный номер: нет.
   
   A 10


   
    A decade update on solvent and catalyst-free neat organic reactions: a step forward towards sustainability [Electronic resource] / A. Sarkar, S. Santra, S. K. Kundu, G. V. Zyryanov, O. N. Chupakhin, V. N. Charushin, A. Majee // Green Chemistry. - 2016. - Vol. 18, № 16. - С. 4475-4525
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ONE-POT SYNTHESIS -- DIELS-ALDER REACTIONS -- ELECTRON-DEFICIENT OLEFINS
Аннотация: Particular success has been achieved in the synthesis of new products and in processes since the twelve principles of "green chemistry" were formulated in the 1990s. These products and processes are more compatible with human health, society, and the environment. In this review, a collection of research reports have been documented from the viewpoint of green chemistry. The main theme of this review is neat reactions, which are solvent and catalyst-free reactions. Neat reactions in the absence of any solvent or catalyst with concise summaries of microwave, ball milling, and neat reactions have been described.

\\\\expert2\\NBO\\Green Chemistry\\2016, v.18, N 16, p.4475.pdf
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9.
Инвентарный номер: нет.
   


   
    Dataset of NMR-spectra pyrrolyl- and indolylazines and evidence of their ability to induce heat shock genes expression in human neurons / E. A. Dutysheva, I. A. Utepova, M. A. Trestsova [et al.] // Data in Brief. - 2021. - № 39. - P107562
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PYRROLYLAZINES -- INDOLYLAZINES -- PHOTOCATALYSIS -- NUCLEAR MAGNETIC RESONANCE -- GREEN CHEMISTRY
Аннотация: These data are related to our previous paper “Synthesis and approbation of new neuroprotective chemicals of pyrrolyl-and indolylazine classes in a cell model of Alzheimer’s disease” (Dutysheva et al., 2021), in which we demonstrate neu-roprotective abilities of pyrrolyl- and indolylazines in a cell model of Alzheimer’s disease. Using a novel procedure of photocatalysis we have synthesized a group of new compounds. The current article presents nuclear magnetic resonance spectra including heteronuclear single quantum coherence spectra of chemicals synthesized by us. The effect of new compounds have on heat shock proteins genes expression in reprogrammed human neurons are presented. We also presented data that verify neuronal phenotype of reprogrammed cells.

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10.
Инвентарный номер: нет.
   


   
    Stimuli-responsive dual cross-linked N-carboxyethylchitosan hydrogels with tunable dissolution rate / S. Bratskaya, A. Skatova, Y. Privar [et al.] // Gels. - 2021. - Vol. 7, № 4. - Ст. 188
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
HYDROGELS -- CHITOSAN -- SALICYLALDEHYDE
Аннотация: Here, we discuss the applicability of (methylenebis(salicylaldehyde)—MbSA) for the fabrication of the stimuli-responsive N-carboxyethylchitosan (CEC) hydrogels with a tunable dissolution rate under physiological conditions. In comparison with non-covalent salicylimine hydrogels, MbSA cross-linking via covalent bis(‘imine clip’) and non-covalent hydrophobic interactions allowed the fabrication of hydrogels with storage moduli > 1 kPa at ten-fold lower aldehyde/CEC molar ratio with the preservation of pH- and amino-acid responsive behavior. Although MbSA-cross-linked CEC hydrogels were stable at neutral and weakly alkaline pH, their disassembly in cell growth medium (Dulbecco’s modified Eagle’s medium, DMEM) under physiological conditions was feasible due to transimination reaction with amino acids contained in DMEM. Depending on the cross-linking density, the complete dissolution time of the fabricated hydrogels varied from 28 h to 11 days. The cytotoxicity of MbSA cross-linked CEC hydrogels toward a human colon carcinoma cell line (HCT 116) and primary human dermal fibroblasts (HDF) was remarkably lower in comparison with CEC-salicylimine hydrogels. Fast gelation, relatively low cytotoxicity, and tunable stimuli-induced disassembly under physiological conditions make MbSA cross-linked CEC hydrogels promising for drug encapsulation and release, 3D printing, cell culturing, and other biomedical applications.

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