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Публикации Чарушина В.Н. (4)

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полный	информационный	краткий

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автору	заглавию	году издания	типу документа

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   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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    Synthesis and antibacterial and antifungal activity of 3-(azol-1-yl)-6-r-1,2,4,5-tetrazines / R. I. Ishmetova, I. A. Belyaninova, A. V. Ignatenko [и др.] // Pharmaceutical chemistry journal. - 2020. - Vol. 53, № 10. - С. 899-904
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
1,2,4,5-TETRAZINES -- 1,3-DIPOLAR CYCLOADDITION -- NUCLEOPHILIC SUBSTITUTION -- ANTIBACTERIAL AND ANTIFUNGAL ACTIVITY
Аннотация: Nucleophilic substitution and 1,3-dipolar cycloaddition reactions were used to synthesize 3,6-disubstituted derivatives of simm-tetrazine containing azolyl, aminoalkyl, and oxyalkyl fragments. The antibacterial activity of the resulting compounds was studied using the obligate pathogen Neisseria gonorrhoeae and opportunistic pathogenic microorganisms, while antifungal activity was assessed using anthropo- and zooanthropophilic dermatophytes.

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   U 61


    Unsymmetrical trifluoromethyl methoxyphenyl β-diketones: effect of the position of methoxy group and coordination at Cu(II) on biological activity / L. A. Khamidullina, I. S. Puzyrev, P. A. Slepukhin [et al.] // Molecules. - 2021. - Vol. 26, № 21. - Ст. 6466

ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
COPPER(II) -- DIKETONATES -- CYTOTOXIC ACTIVITY -- ANTIMICROBIAL ACTIVITY
Аннотация: Copper(II) complexes with 1,1,1-trifluoro-4-(4-methoxyphenyl)butan-2,4-dione (HL1) were synthesized and characterized by elemental analysis, FT-IR spectroscopy, and single crystal X-ray diffraction. The biological properties of HL1 and cis-[Cu(L1)2(DMSO)] (3) were examined against Gram-positive and Gram-negative bacteria and opportunistic unicellular fungi. The cytotoxicity was estimated towards the HeLa and Vero cell lines. Complex 3 demonstrated antibacterial activity towards S. aureus comparable to that of streptomycin, lower antifungal activity than the ligand HL1 and moderate cytotoxicity. The bioactivity was compared with the activity of compounds of similar structures. The effect of changing the position of the methoxy group at the aromatic ring in the ligand moiety of the complexes on their antimicrobial and cytotoxic activity was explored. We propose that complex 3 has lower bioavailability and reduced bioactivity than expected due to strong intermolecular contacts. In addition, molecular docking studies provided theoretical information on the interactions of tested compounds with ribonucleotide reductase subunit R2, as well as the chaperones Hsp70 and Hsp90, which are important biomolecular targets for antitumor and antimicrobial drug search and design. The obtained results revealed that the complexes displayed enhanced affinity over organic ligands. Taken together, the copper(II) complexes with the trifluoromethyl methoxyphenyl-substituted β-diketones could be considered as promising anticancer agents with antibacterial properties

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    Synthesis, fungicidal activity, and molecular docking of 2-acylamino and 2-thioacylamino derivatives of 1 H-benzo[ d]imidazoles as anti-tubulin agents / K. L. Obydennov, T. A. Kalinina, N. A. Galieva [et al.] // Journal of agricultural and food chemistry. - 2021. - Vol. 69, № 40. - P12048-12062
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
BENZIMIDAZOLES -- ANTIFUNGAL ACTIVITY -- TUBULIN -- CARBENDAZIM
Аннотация: This work deals with the synthesis and evaluation of fungicidal activity of benzimidazole derivatives, which are structural analogues of commercial anti-tubulin fungicides. A number of N-acyl and N-thioacyl derivatives of 2-amino-1H-benzo[d]imidazole were prepared, and their fungicidal activity against 13 strains of phytopathogenic fungi was studied. The most active compounds against the majority of the studied strains were 3a, 4l, and 4o, and the EC50 values of these compounds were in the range 2.5–20 μg/mL. Compound 3a showed the highest activity against the P. infestans strain, the growth of which is not suppressed by carbendazim. The formation of ligand–receptor complexes of various tautomeric forms of the studied benzimidazoles with homologous models of β-tubulins of B. cinerea, F. oxysporum, and P. infestans was modeled. Induced fit docking has been used for the simulation. The obtained data suggest the possibility of binding of benzimidazole fungicides to β-tubulin in the ″nocodazole cavity″ in the tautomeric form bearing a double exocyclic C═N bond. The importance of the formation of hydrogen bonds of benzimidazoles with the amino acid residue Val236 along with the Glu198 residue is also revealed in the present study.

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    Promising antifungal and antibacterial agents based on 5-aryl-2,2'-bipyridines and their heteroligand salicylate metal complexes: synthesis, bioevaluation, molecular docking / Y. V. Burgart, E. V. Shchegolkov, I. V. Shchur [et al.] // Chemmedchem: chemistry enabling drug discovery. - 2022. - Vol. 17, № 3. - Pe202100577
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: A series of new 5-aryl-2,2′-bipyridines and their (polyfluoro)salicylate metal complexes was synthesized. Their antimicrobial activity was evaluated in vitro against eight strains of dermatophytes, seven strains of Candida yeasts, eight strains of Gram-positive and two strains of Gram-negative bacteria. Using molecular docking, we proposed that anti-staphylococcal action proceeds through the inhibition mechanism of the leading compounds to S. aureus DNA gyrase GyrB.

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    Azolyl pyrimidines-synthesis and antimicrobial activity / N. H. Basha, T. Rekha, V. Padmavathi [et al.] // AIP conference proceedings. - 2022. - Vol. 2390. - Ст. 020006
Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ
   ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
CHEMICAL COMPOUNDS -- PHARMACEUTICALS -- ANTIMICROBIALS
Аннотация: Amide unit is a privileged structural motif and is a constituent of proteins, natural products and pharmaceuticals. Amongst different heterocyclic scaffolds, azoles and pyrimidines are the prominent entities in pharmaceutical arena. The biopotency of these heterocycles have triggered to synthesize a variety of heteroaromatics – azoles linked with pyridines by amino acetamide group. The target molecules-azolylaminoacetamidopyrimidines were prepared by the reaction of methyl azolylglycinate with pyrimidinyl-2-amine in the presence of DMAP and triethylamine in dichloromethane under ultrasonication. The lead molecules were evaluated for antimicrobial activity. Nitro substituted 2-((4-(4-chlorofuran-2-yl)thiazole-2-yl)amino)-N-(4,6-diphenylpyrimidin-2-yl)acetamide (9c) displayed excellent antibacterial activity against B. subtilis greater than the standard drug Chloramphenicol. However, 9c and nitro substituted 2-((4-(4-chlorofuran-2-yl)-1H-imidazol-2-yl)amino)-N-(4,6-diphenylpyrimidin-2-yl)acetamide (10c) showed antifungal activity on A. niger greater than the standard drug Ketoconazole.

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    Bis(azolyl)sulfonamidoacetamides: Synthesis and bioassay / P. S. Sankar, K. N. Babu, V. N. Padmavathi [et al.] // AIP conference proceedings. - 2022. - Vol. 2390. - Ст. 020021
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ANTIMICROBIALS -- BIOASSAYS -- ANTIFUNGAL
Аннотация: Azole derivatives are valuable precursors in pharmacological arena. In fact, oxazole, thiazole and imidazole containing scaffolds display a variety of biological activities such as antitumor,1 antibacterial,2 antiviral,3 antioxidant,4,5 anti-inflammatory6 and antifungal7 activities. Azoles are also prominant molecules in various biochemical and synthetic transformations. Based on the importance of these heteroaromatics and also our interest to link the heterocycle molecules with a variety of functional groups we have synthesized a new class of bis(azolyl)sulfonamide acetamides from azolylsulfonylamines and azolylchloroacetamides in the presence of DMAP under ultrasonication and studied their antimicrobial activity. The compounds chloro substituted bis(thiazoles) (6c) and chloro substituted imidazolyl thiazoles (7c) displayed excellent antibacterial activity against B. subtilis greater than the standard drug, Chloramphenicol. Whereas 7c also showed excellent antifungal activity on A. niger higher than the standard drug, Ketoconazole.

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    Synthesis and biological evaluation of polyfluoroalkyl-containing 4-arylhydrazinylidene-isoxazoles as antifungal agents with antioxidant activity / N. A. Elkina, E. V. Shchegolkov, Y. V. Burgart [и др.] // Journal of Fluorine Chemistry. - 2022. - Vol. 254. - Ст. 109935
Рубрики: ХИМИЧЕСКИЕ НАУКИ

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    Facile synthesis of 6-organyl-4-(trifluoromethyl)pyridin-2(1H)-ones and their polyfluoroalkyl-containing analogs / S. O. Kushch, M. V. Goryaeva, Ya. V. Burgart [et al.] // Russian chemical bulletin. - 2022. - Vol. 71, № 8. - P1687-1700
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The three-component cyclization of 3-polyfluoroalkyl-3-oxopropanoates and methyl ketones with ammonium acetate affords 6-organyl-4-(polyfluoroalkyl)pyridin-2(1H)-ones (organyl is alkyl, aryl, or hetaryl). The synthesized pyridones were evaluated for antifungal, antibacterial, and analgesic activity.

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