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1.

Вид документа : Статья из журнала
Шифр издания :
Автор(ы) : Dutysheva E. A., Utepova I. A., Trestsova M. A., Anisimov A. S., Charushin V. N., Chupakhin O. N., Margulis B. A., Guzhova I. V., Lazarev V. F.
Заглавие : Dataset of NMR-spectra pyrrolyl- and indolylazines and evidence of their ability to induce heat shock genes expression in human neurons
Место публикации : Data in Brief. - 2021. - № 39. - С. 107562
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): 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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2.

Вид документа : Статья из журнала
Шифр издания :
Автор(ы) : Dutysheva E. A., Utepova I. A., Trestsova M. A., Anisimov A. S., Charushin V. N., Chupakhin O. N., Margulis B. A., Guzhova I. V., Lazarev V. F.
Заглавие : Synthesis and approbation of new neuroprotective chemicals of pyrrolyl- and indolylazine classes in a cell model of Alzheimer's disease
Место публикации : European journal of medicinal chemistry. - 2021. - Vol. 222. - С. 113577
Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ
Ключевые слова (''Своб.индексиров.''): pyrrolylazines--neuroprotectors--chaperones--amyloid-beta--alzheimer's disease
Аннотация: One of the major causes of neurodegeneration in the pathogenesis of Alzheimer's disease is the accumulation of cytotoxic amyloid species within the intercellular compartments of the brain. The efficacy of the anti-proteotoxic mechanism based on the molecular chaperones Hsp70 and Hsp90 in numerous types of neurons is often low, while its pharmacological enhancement has been shown to ameliorate the physiological and cognitive functions of the brain. Suggesting that the chemicals able to induce heat shock protein synthesis and therefore rescue neural cells from cytotoxicity associated with amyloid, we have synthesized a group of pyrrolyl- and indolylazines that cause the accumulation of heat shock proteins, using a novel method of photocatalysis that is employed in green chemistry. The selected compounds were tested in a cell model of Alzheimer's disease and demonstrated a pronounced neuroprotective effect. These substances increased the survival of neurons, blocked the activation of β-galactosidase, and prevented apoptosis in neurons cultured in the presence of β-amyloid.
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3.

Вид документа : Статья из журнала
Шифр издания :
Автор(ы) : Dutysheva E. A., Mikeladze M. A., Aksenov N. D., Mikhaylova E. R., Suezov R. V., Guzhova I. V., Margulis B. A., Lazarev V. F., Trestsova M. A., Utepova I. A., Charushin V. N., Chupakhin O. N.
Заглавие : Pyrrolylquinoxaline-2-one derivative as a potent therapeutic factor for brain trauma rehabilitation
Место публикации : Pharmaceutics. - 2020. - Vol. 12, № 5. - С. 414
Ключевые слова (''Своб.индексиров.''): apoptosis--cerebrospinal fluid--hsp70--small molecule--traumatic brain injury
Аннотация: Traumatic brain injury (TBI) often causes massive brain cell death accompanied by the accumulation of toxic factors in interstitial and cerebrospinal fluids. The persistence of the damaged brain area is not transient and may occur within days and weeks. Chaperone Hsp70 is known for its cytoprotective and antiapoptotic activity, and thus, a therapeutic approach based on chemically induced Hsp70 expression may become a promising approach to lower post-traumatic complications. To simulate the processes of secondary damage, we used an animal model of TBI and a cell model based on the cultivation of target cells in the presence of cerebrospinal fluid (CSF) from injured rats. Here we present a novel low molecular weight substance, PQ-29, which induces the synthesis of Hsp70 and empowers the resistance of rat C6 glioma cells to the cytotoxic effect of rat cerebrospinal fluid taken from rats subjected to TBI. In an animal model of TBI, PQ-29 elevated the Hsp70 level in brain cells and significantly slowed the process of the apoptosis in acceptor cells in response to cerebrospinal fluid action. The compound was also shown to rescue the motor function of traumatized rats, thus proving its potential application in rehabilitation therapy after TBI.
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4.

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
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5.

Вид документа : Статья из журнала
Шифр издания : 54/B 78
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
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6.

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.
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7.

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
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8.

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
\\\\expert2\\nbo\\Antimicrobal Agents and Chemotherapy\\2010. V. 54, N 5. P. 2017-2022.pdf
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9.

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
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10.

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
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11.

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
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12.

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
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