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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 [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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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 [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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4.
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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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.
   
   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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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.
   


   
    Asymmetrically substituted 5,5′′-diaryl-2,2′:6′,2′′-terpyridines as efficient fluorescence “turn-on” probes for Zn2+ in food/cosmetic samples and human urine / O. V. Shabunina, E. S. Starnovskaya, Y. K. Shaitz [et al.] // Journal of photochemistry and photobiology A: Chemistry. - 2021. - Vol. 408. - P113101
Рубрики: ХИМИЧЕСКИЕ НАУКИ

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10.
Инвентарный номер: нет.
   


   
    Synthesis, characterization, and in vitro assessment of cytotoxicity for novel azaheterocyclic nido-carboranes – Candidates in agents for boron neutron capture therapy (BNCT) of cancer / M. V. Varaksin, L. A. Smyshliaeva, V. L. Rusinov [et al.] // Tetrahedron. - 2021. - Vol. 102. - P132525
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
AZAHETEROCYCLES -- BNCT -- CYTOTOXICITY -- CARBORANES
Аннотация: A series of novel water-soluble azaheterocyclic derivatives of nido-carborane bearing quinoxaline, 2H-imidazole or 1,2,4-triazine moieties were first synthesized in 82–91% yields. The structures of these boron-enriched compounds were confirmed by the data of NMR, IR spectroscopy, and mass spectrometry. To access the toxicity level for these organoboron compounds, the cytotoxicity indexes (IC50) were determined using by the MTT test on both human glioblastoma cell A-172 (IC50 = 150–243 μM) and human embryonic lung cells (IC50 = 424–944 μM) lines. The obtained preliminary results from in vitro analysis enable the synthesized water-soluble azaheterocyclic carboranes to be considered as challenging candidates in the design of agents for boron-neutron capture therapy (BNCT) of malignant tumors.

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