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 Найдено в других БД:Публикации Чарушина В.Н. (9)
Формат представления найденных документов:
полныйинформационныйкраткий
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авторузаглавиюгоду изданиятипу документа
Поисковый запрос: (<.>K=ANTIMYCOBACTERIAL<.>)
Общее количество найденных документов : 10
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1.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis and antimycobacterial activity of enantiomerically pure 1-ethyl-2,3-dicyano-5-(het)aryl-6-hetaryl-1,6-dihydropyrazines / E. V. Verbitskiy, M. A. Kravchenko, I. D. Medvinskiy, G. L. Rusinov, V. N. Charushin // Уральский научный форум "Современные проблемы органической химии". XVII Молодежная школа-конф. по органической химии, Екатернинбург, 8-12 июня 2014 г. : сб. тез. - Екатеринбург, 2014. - С. 48
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
SYNTHESIS -- ANTIMICOBACTERIAL ACTIVITY

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2.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis, X-ray crystal structure and antimycobacterial activity of enantiomerically pure 1-ethyl-2,3-dicyano-5-(het)aryl-6-hetaryl-1,6-dihydropyrazines / E. V. Verbitskiy, M. S. Toropova, M. I. Kodess, M. A. Ezhikova, M. I. Isenov, M. G. Pervova, M. A. Kravchenko, I. D. Medvinskiy, S. N. Skornyakov, G. L. Rusinov, V. N. Charushin // ARKIVOC. - 2014. - Pt. V. - С. 247-270
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
X-RAY CRYSTAL -- ANTIMYCOBACTERIAL ACTIVITY -- SYNTHESIS

\\\\expert2\\nbo\\ARKIVOC\\2014, p.247-270.pdf
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3.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis, and structure-activity relationship for C(4) and/or C(5) thienyl substituted pyrimidines, as a new family of antimycobacterial compounds [Electronic resource] / E. V. Verbitskiy, E. M. Cherprakova, P. A. Slepukhin, M. A. Kravchenko, S. N. Skornyakov, G. L. Rusinov, O. N. Chupakhin, V. N. Charushin // European Journal of Medicinal Chemisrty. - 2015. - Vol. 96. - С. 225-234. - Bibliogr. : p. 234 (36 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ

\\\\expert2\\nbo\\European Journal of Medicinal Chemistry\\2015, v.96, p.225-234.pdf
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4.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis, antimycobacterial and antifungal evaluation of some new 1-ethyl-5-(hetero)aryl-6-styryl-1,6-dihydropyrazine-2,3-dicarbonitriles [Electronic resource] / E. V. Verbitskiy, P. A. Slepukhin, M. A. Kravchenko, S. N. Skornyakov, N. P. Evstigneeva, N. V. Kungurov, N. V. Zil'berberg, G. L. Rusinov, O. N. Chupakhin, V. N. Charushin // Bioorganic and Medicinal Chemistry Letters. - 2015. - Vol. 25, № 3. - С. 524-528. - Bibliogr. : p. 528 (16 ref.)
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PYRAZINES -- ANTITUBERCULOSIS ACTIVITY -- PETASIS REACTION
Аннотация: The Petasis reaction of 6-hydroxy adducts of 1-alkyl-2,3-dicyano-5-arylpyrazinium salts with trans-styrylboronic acids proved to proceed smoothly at room temperature to give the corresponding 5-(hetero)aryl-6-styryl substituted 1,6-dihydropyrazine derivatives. Also it has been found that C(6) unsubstituted 1,6-dihydro- or 1,4,5,6-tetrahydropyrazine derivatives can be easy prepared in high yields from the corresponding pyrazinium salts by reduction with triethylsilane. All synthesized compounds were screened in vitro for their antifungal activities against seven pathogenic fungal strains and antimycobacterial activities against Mycobacterium tuberculosis H(37)Rv, avium, terrae and multi-drug-resistant strains isolated from tuberculosis patients in the Ural region (Russia)

\\\\expert2\\nbo\\Bioorganic and Medicinal Chemistry Letters\\2015, v. 25, p. 524.pdf
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5.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis of new C(4) and/or C(5) thienyl substituted pyrimidines as potential antimycobacterial agents. / E. V. Verbitskiy, E. M. Cheprakova, M. A. Kravchenko, S. N. Skornyakov, G. L. Rusinov, O. N. Chupakhin, V. N. Charushin // 19h European Symposium on Organic Chemistry (ESOC-2015), 12th-16th July, Lisboa, Portugal, 2015. : book of abstr. . - Lisboa, 2015. - С. 450
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PYRIMIDINES -- ANTIMYCOBACTERIAL AGENTS -- SYNTHESIS

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6.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines [Электронный ресурс] / E. V. Verbitskiy, S. A. Baskakova, M. A. Kravchenko, S. N. Skornyakov, G. L. Rusinov, O. N. Chupakhin, V. N. Charushin // Bioorganic and Medicinal Chemistry. - 2016. - Vol. 24, № 16. - С. 3771-3780
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PYRIMIDINE -- ANTIMYCOBACTERIAL ACTIVITY -- TUBERCULOSIS
Аннотация: Various 5-(fluoroaryl)-4-(hetero)aryl substituted pyrimidines have been synthesized based on the Suzuki cross-coupling and nucleophilic aromatic substitution of hydrogen (S-N(H)) reactions starting from commercially available 5-bromopyrimidine and their antitubercular activity against Mycobacterium tuberculosis H(37)Rv has been explored. The outcome of the study disclose that, some of the compounds have showed promising activity in micromolar concentration against Mycobacterium tuberculosis H(37)Rv, Mycobacterium avium, Mycobacterium terrae, and multidrug-resistant strains isolated from tuberculosis patients in Ural region (Russia). The data concerning the 'structure-activity' relationship for fluorinated compounds have been discussed

\\\\expert2\\NBO\\Bioorganic and Medicinal Chemistry\\2016, V.24, N 16, p.3771-3780.pdf
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7.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis and antimycobacterial activity of N-(2-aminopurin-6-yl) and N-(purin-6-yl) amino acids and dipeptides [Electronic resource] / V. P. Krasnov, A. Yu. Vigorov, V. V. Musiyak, I. A. Nizova, D. A. Gruzdev, T. V. Matveeva, G. L. Levit, V. N. Charushin // Bioorganic and Medicinal Chemistry Letters. - 2016. - Vol. 26, № 11. - С. 2645-2648
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PURINE -- GLUTAMIC ACID -- AMINO ACIDS
Аннотация: Synthetic routes to novel N-(purin-6-yl)- and N-(2-aminopurin-6-yl) conjugates with amino acids and glycine-containing dipeptides were developed. In vitro testing of 42 new and known compounds made it possible to reveal a series of N-(purin-6-yl)- and N-(2-aminopurin-6-yl) conjugates exhibiting significant antimycobacterial activity against Mycobacterium tuberculosis H37Rv, Mycobacterium avium, Mycobacterium terrae, and multidrug-resistant M. tuberculosis strain isolated from tuberculosis patients in the Ural region (Russia). N-(2-Aminopurin-6-yl)- and N-(purin-6-yl)-glycyl-(S)-glutamic acids were the most active compounds. (C) 2016 Elsevier Ltd. All rights reserved

\\\\expert2\\NBO\\Bioorganic and Medicinal Chemistry Letters\\2016, v. 26, p. 2645.pdf
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8.
Инвентарный номер: нет.
   
   S 98


   
    Synthesis and biological evaluation of novel 5-aryl-4-(5-nitrofuran-2-yl)-pyrimidines as potential anti-bacterial agents / E. V. Verbitskiy [et al.] // Bioorganic and Medicinal Chemistry Letters. - 2017. - Vol. 27, № 13. - P3003-3006
ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
PYRIMIDINE -- NITROFURAN -- ANTIGONORRHEAL -- ANTIMYCOBACTERIAL -- NUCLEOPHILIC AROMATIC SUBSTITUTION OF HYDROGEN
Аннотация: A facile two-step synthetic approach to fluorinated and non-fluorinated 5-aryl-4-(5-nitrofuran-2-yl)-pyrimidines from readily available 5-bromo-4-(furan-2-yl)pyrimidine has been developed. All synthesized compounds were screened in vitro for their antibacterial activities against twelve various bacterial strains. It is demonstrated that some of these compounds exhibited significant antibacterial activities against strains Neisseria gonorrhoeae and Staphylococcus aureus, comparable and even higher with that commercial drug Spectinomycin.

\\\\Expert2\\NBO\\Bioorganic and Medicinal Chemistry Letters\\2017 v.27 p.3003-3006.pdf
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9.
Инвентарный номер: нет.
   
   S 83


   
    Stereochemical aspects in the synthesis of novel N-(purin-6-yl)dipeptides as potential antimycobacterial agents / V. V. Musiyak, I. A. Nizova, E. N. Chulakov [et al.] // Amino Acids. - 2021. - Vol. 53, № 3. - P407-415
ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
DIPEPTIDES -- RACEMIZATION -- PURINE -- COUPLING -- NUCLEOPHILIC SUBSTITUTION -- ANTIMYCOBACTERIAL ACTIVITY
Аннотация: The synthesis of purine conjugates with natural amino acids is one of the promising directions in search for novel therapeutic agents, including antimycobacterial agents. The purpose of this study was to synthesize N-(purin-6-yl)dipeptides containing the terminal fragment of (S)-glutamic acid. To obtain the target compounds, two synthetic routes were tested. The first of them is based on coupling of N-(purin-6-yl)-(S)-amino acids to dimethyl (S)-glutamate in the presence of carbodiimide coupling agent followed by the removal of ester groups. However, it turned out that this coupling process was accompanied by racemization of the chiral center of N-(purin-6-yl)-α-amino acids and in all cases led to mixtures of (S,S)- and (R,S)diastereomers (6:4). Individual (S,S)-diastereomers were obtained using an alternative approach based on the nucleophilic substitution of chlorine in 6-chloropurine or 2-amino-6-chloropurine with corresponding dipeptides as nucleophiles. The enantiomeric purity of the target compounds was confirmed by chiral HPLC. To test the assumption that racemization of the chiral center of N-(purin-6-yl)-α-amino acids occurs with the participation of nitrogen atoms of the imidazole ring via the stage of formation of a chirally labile intermediate, we obtained such structural analogs of N-(purin-6-yl)-(S)-alanine as N-(9-benzylpurin-6-yl)-(S)-alanine and N-(7-deazapurin-6-yl)-(S)-alanine. It was found that coupling of these compounds to dimethyl (S)-glutamate was also accompanied by racemization. This indicates that the imidazole fragment does not play a crucial role in this process. When testing the antimycobacterial activity of some of the obtained compounds, conjugates with moderate activity against the laboratory Mycobacterium tuberculosis H37Rv strain (MIC 3.1–6.25 μg/mL) were identified.

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10.
Инвентарный номер: нет.
   


   
    New approach to biologically active indolo[2,3-b]quinoxaline derivatives through intramolecular oxidative cyclodehydrogenation / G. Sadykhov, D. V. Belyaev, M. G. Pervova [et al.] // ChemistrySelect. - 2022. - Vol. 7, № 18. - Pe202200497
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: A convenient synthetic protocol to antiviral agent B-220 and a series of similar indolo[2,3-b]quinoxaline derivatives has been developed. This synthetic approach is based on Buchwald-Hartwig cross-coupling and subsequent annulation by intramolecular oxidative cyclodehydrogenation. For the first time, 6H-indolo[2,3-b]quinoxaline amine derivatives were evaluated for antimycobacterial activity. The moderate bacteriostatic effect against Mycobacterium tuberculosis H37Rv was found. A plausible mechanism of antibacterial action was elucidated by the molecular docking.

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