Центральная Научная Библиотека УрО РАН

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   S 98


    Synthesis and tuberculostatic activity of fluoridized 3-Z-hydrazine-2-benzoyl acrylates and their cyclization products / M. A. Kravchenko, E. V. Nosova, G. N. Lipunova, O. M. Chasovskikh, V. A. Sokolov, V. N. Charushin // Problemy tuberkuleza . - 2003. - №7. - С. 49-52

ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ACRYLIC ACID DERIVATIVE -- PYRAZOLE -- TUBERCULOSTATIC AGENT
Аннотация: A rapid development of the resistance of drugs and their toxic and adverse reactions suggest that new antituberculous drugs should be designed. Of the greatest importance is isoniazid resistance. Testing new compounds (IIa, b) has established that the minimum inhibitory concentration of the drug (IIa), 0.39 microgram/ml suppresses the growth of Mycobacterium tuberculosis (MBT) in the macrophages up to 50%, that of the drug (IIb), 1.56 micrograms/ml, causes death in 25% of cases, which is indicative of the high activity of compounds (IIa, b) against MBT

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   S 98


    Synthesis and antitumour activity of 4-aminoquinazoline derivatives [Electronic resource] / G. N. Lipunova, E. V. Nosova, V. N. Charushin, O. N. Chupakhin // Russian Chemical Reviews. - 2016. - Vol. 85, № 7. - С. 759-793

ББК 54
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
GROWTH-FACTOR RECEPTOR -- POTENT EGFR INHIBITORS -- TYROSINE KINASE INHIBITORS
Аннотация: Scieces of data on the synthesis and antitumour activity of 4-aminoquinazolines are summarized and analyzed. Key methods for the synthesis of these compounds are considered, primarily cyclocondensation of carboxylic acid derivatives, as well as the oxidation of quinazolines and the cyclization of disubstituted thioureas. Improvements of synthetic schemes for erlotinib, gefitinib and lapatinib, which are the best-known pharmaceuticals based on compounds of the title class, are also considered. Synthetic strategies and biological activities for new 4-aminoquinazoline derivatives that are EGFR-tyrosine kinase inhibitors, multiactive compounds, and labelled compounds for use as positron emission tomography (PET) imaging agents are discussed.

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    Synthesis and physicochemical and catalytic properties of composites in the Sio2–Zro2 system / A. N. Murashkevich, O. A. Alisienok, E. S. Novik [et al.] // Inorganic materials. - 2020. - Vol. 56, № 4. - P430-436
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
ACID-BASE PROPERTIES -- CATALYSIS -- COMPOSITE -- SILICA -- SPECIFIC SURFACE AREA -- ZIRCONIA
Аннотация: Using coprecipitation, a sol–sol method, and molecular layering, we have synthesized SiO2–ZrO2 composites with SiO2 : ZrO2 ratios from 1 : 1 to 9 : 1 and a large specific surface area, which increases with growth silicon-containing component concentration. Using adsorption of Hammett indicators, we have assessed the concentration of acid–base centers in the pK range 1.3–9.6, which has been shown to vary from 68 to 160 μmol/g. Elemental analysis and IR spectroscopy data have demonstrated the presence of not only water but also nitrate ions and carbon dioxide on the surface of the samples. It has been shown that the use of nanoparticulate SiO2–ZrO2 oxides as heterogeneous catalysts—promoters for (2S,4R)-4-hydroxyprolyl-(S)-1-phenylethylamine trifluoroacetate, a chiral inducer in the asymmetric Biginelli reaction, makes it possible to raise ee (enantiomeric excess) from 39 to 68% and the reaction yield from 29 to 55%.

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