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1.
Stalinskaya A. L. Shulgau Z. T. Sergazy Sh. D. Gulyaev A. E. Turdybekov D. M. Turdybekov K. M. Kulakov I. V. 《Russian Journal of General Chemistry》2022,92(2):147-153
Russian Journal of General Chemistry - A three-component reaction of 3,5-diacetyl-2,6-dimethylpyridine, p-N-dimethylaminobenzaldehyde and phenylhydrazine in the presence of KOH in ethanol gave the... 相似文献
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Lyudmila Kayukova Anna Vologzhanina Pavel Dorovatovskii Gulnur Baitursynova Elmira Yergaliyeva Ayazhan Kurmangaliyeva Zarina Shulgau Sergazy Adekenov Zhanar Shaimerdenova Kydymolla Akatan 《Molecules (Basel, Switzerland)》2022,27(7)
Nitrobenzenesulfochlorination of β-aminopropioamidoximes leads to a set of products depending on the structure of the initial interacting substances and reaction conditions. Amidoximes, functionalized at the terminal C atom with six-membered N-heterocycles (piperidine, morpholine, thiomorpholine and phenylpiperazine), as a result of the spontaneous intramolecular heterocyclization of the intermediate reaction product of an SN2 substitution of a hydrogen atom in the oxime group of the amidoxime fragment by a nitrobenzenesulfonyl group, produce spiropyrazolinium ortho- or para-nitrobenzenesulfonates. An exception is ortho-nitrobenzenesulfochlorination of β-(thiomorpholin-1-yl)propioamidoxime, which is regioselective at room temperature, producing two spiropyrazolinium salts (ortho-nitrobezenesulfonate and chloride), and regiospecific at the boiling point of the solvent, when only chloride is formed. The para-Nitrobezenesulfochlorination of β-(benzimidazol-1-yl)propioamidoxime, due to the reduced nucleophilicity of the aromatic β-amine nitrogen atom, is regiospecific at both temperatures, and produces the O-para-nitrobenzenesulfochlorination product. The antidiabetic screening of the new nitrobezenesulfochlorination amidoximes found promising samples with in vitro α-glucosidase activity higher than the reference drug acarbose. 1H-NMR spectroscopy and X-ray analysis revealed the slow inversion of six-membered heterocycles, and experimentally confirmed the presence of an unfavorable stereoisomer with an axial N–N bond in the pyrazolinium heterocycle. 相似文献
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Palamarchuk I. V. Shulgau Z. T. Sergazy Sh. D. Zhulikeeva A. M. Seilkhanov T. M. Kulakov I. V. 《Russian Journal of General Chemistry》2022,92(9):1692-1705
Russian Journal of General Chemistry - On the basis of 4-(thien-2-yl)-3-aminopyridine-2(1H)-one, the corresponding chloroacetamide and condensed 1H-pyrido[2,3-b][1,4]oxazine-2(3H)-one were... 相似文献
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Alena L. Stalinskaya Nadezhda V. Martynenko Zarina T. Shulgau Alexandr V. Shustov Viktoriya V. Keyer Ivan V. Kulakov 《Molecules (Basel, Switzerland)》2022,27(12)
The COVID-19 pandemic is ongoing as of mid-2022 and requires the development of new therapeutic drugs, because the existing clinically approved drugs are limited. In this work, seven derivatives of epoxybenzooxocinopyridine were synthesized and tested for the ability to inhibit the replication of the SARS-CoV-2 virus in cell cultures. Among the described compounds, six were not able to suppress the SARS-CoV-2 virus’ replication. One compound, which is a derivative of epoxybenzooxocinopyridine with an attached side group of 3,4-dihydroquinoxalin-2-one, demonstrated antiviral activity comparable to that of one pharmaceutical drug. The described compound is a prospective lead substance, because the half-maximal effective concentration is 2.23 μg/μL, which is within a pharmacologically achievable range. 相似文献
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Oleshchuk Alena L. Karbainova Anastasiya A. Krivoruchko Tatyana N. Shulgau Zarina T. Seilkhanov Tulegen M. Kulakov Ivan V. 《Chemistry of Heterocyclic Compounds》2019,55(1):47-51
Chemistry of Heterocyclic Compounds - Aldol-crotonic condensation reactions of 3,5-diacetyl-2,6-dimethylpyridine with various aldehydes were used to synthesize bisazachalcone derivatives, which... 相似文献
8.
Shynggys Sergazy Zarina Shulgau Aigerim Zhulikeyeva Yerlan Ramankulov Irina V. Palamarchuk Ivan V. Kulakov 《Molecules (Basel, Switzerland)》2022,27(17)
Currently, studies are being conducted on the possible role of the cytoprotective effect of biologically active substances in conditions of cerebral hypoxia or cardiomyopathies. At the same time, oxidative stress is considered one of the important mechanisms of cellular cytotoxicity and a target for the action of cytoprotectors. The aim of this study is to search for derivatives of 3-(arylmethylamino)-6-methyl-4-phenylpyridin-2(1H)-ones. The probability of cytoprotective action was assessed by measuring cell viability using two tests (with neutral red dye and MTT test). It was found that some derivatives of 3-(arylmethylamino)-6-methyl-4-phenylpyridin-2(1H)-ones under the conditions of our experiment had a pronounced cytoprotective activity, providing better cell survival in vitro, including the MTT test and conditions of blood hyperviscosity. To correlate the obtained results in vitro, molecular docking of the synthesized derivatives was also carried out. The standard drug omeprazole (co-crystallized with the enzyme) was used as a standard. It was shown that all synthesized derivatives of 3-(arylmethylamino)-6-methyl-4-phenylpyridin-2(1H)-ones had higher affinity for the selected protein than the standard gastro-cytoprotector omeprazole. The studied derivatives of 3-(arylmethylamino)-6-methyl-4-phenylpyridin-2(1H)-ones also fully satisfy Lipinski’s rule of five (RO5), which increases their chances for possible use as orally active drugs with good absorption ability and moderate lipophilicity. Thus, the results obtained make it possible to evaluate derivatives of 3-(arylmethylamino)-6-methyl-4-phenylpyridin-2(1H)-ones as having a relatively high cytoprotective potential. 相似文献
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Koveza Vladislav A. Kulakov Ivan V. Shulgau Zarina T. Seilkhanov Tulegen M. 《Chemistry of Heterocyclic Compounds》2018,54(12):1127-1130
Chemistry of Heterocyclic Compounds - Reaction of 2-nitroacetophenone, furfurol, β-dicarbonyl compounds, and ammonium acetate led to 3-substituted... 相似文献
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Kulakov I. V. Shulgau Z. T. Turdybekov K. M. Turdybekov D. M. Sadyrbekov D. T. 《Russian Journal of General Chemistry》2015,85(2):467-471
Russian Journal of General Chemistry - New 5,6-dihydro-1,3-thiazin-4-one derivatives have been synthesized by one-pot reaction of morpholin-4-amine and adamantan-1-amine with methacryloyl... 相似文献