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Mikhail V. Pugachev Nikita V. Shtyrlin Lubov P. Sysoeva Elena V. Nikitina Timur I. Abdullin Alfiya G. Iksanova Alina A. Ilaeva Rashid Z. Musin Eugeny A. Berdnikov Yurii G. Shtyrlin 《Bioorganic & medicinal chemistry》2013,21(14):4388-4395
A series of 13 phosphonium salts on the basis of pyridoxine derivatives were synthesized and their antibacterial activity against clinically relevant strains was tested in vitro. All compounds were almost inactive against gram-negative bacteria and exhibited structure-dependent activity against gram-positive bacteria. A crucial role of ketal protection group in phosphonium salts for their antibacterial properties was demonstrated. Among synthesized compounds 5,6-bis[triphenylphosphonio(methyl)]-2,2,8-trimethyl-4H-[1,3]dioxino[4,5-c]pyridine dichloride (compound 20) was found to be the most effective towards Staphylococcus aureus and Staphylococcus epidermidis strains (MIC 5 μg/ml). The mechanism of antibacterial activity of this compound probably involves cell penetration and interaction with genomic and plasmid DNA. 相似文献
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Shtyrlin Valery G. Borissenok Valery A. Serov Nikita Yu. Simakov Vladimir G. Bragunets Vyacheslav A. Trunin Ivan R. Tereshkina Irina A. Koshkin Sergey A. Bukharov Mikhail S. Gilyazetdinov Edward M. Shestakov Evgeny E. Sirotkina Anna G. Zakharov Alexey V. 《Origins of life and evolution of the biosphere》2019,49(1-2):1-18
Origins of Life and Evolution of Biospheres - Syntheses under shock in nitrogen bubbled samples of the water – formamide – bicarbonate – sodium hydroxide system at... 相似文献
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Amino Acids - The kinetics of oligopeptides formation in the flow systems glycine–sodium trimetaphosphate–imidazole/N-methylimidazole at thermocyclic regime has been investigated by... 相似文献
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Mikhail V. Pugachev Nikita V. Shtyrlin Sergey V. Sapozhnikov Lubov P. Sysoeva Alfiya G. Iksanova Elena V. Nikitina Rashid Z. Musin Olga A. Lodochnikova Eugeny A. Berdnikov Yurii G. Shtyrlin 《Bioorganic & medicinal chemistry》2013,21(23):7330-7342
A series of 23 novel bis-phosphonium salts based on pyridoxine were synthesized and their antibacterial activities were evaluated in vitro. All compounds were inactive against gram-negative bacteria and exhibited the structure-dependent activity against gram-positive bacteria. The antibacterial activity enhanced with the increase in chain length at acetal carbon atom in the order n-Pr > Et > Me. Further increasing of length and branching of alkyl chain leads to the reduction of antibacterial activity. Replacement of the phenyl substituents at the phosphorus atoms in 5,6-bis(triphenylphosphonio(methyl))-2,2,8-trimethyl-4H-[1,3]-dioxino[4,5-c]pyridine dichloride (compound 1) with n-butyl, m-tolyl or p-tolyl as well as chloride anions in the compound 1 with bromides (compound 14a) increased the activity against Staphylococcus aureus and Staphylococcus epidermidis up to 5 times (MICs = 1–1.25 μg/ml). But in practically all cases chemical modifications of compound 1 led to the increase of its toxicity for HEK-293 cells. The only exception is compound 5,6-bis[tributylphosphonio(methyl)]-2,2,8-trimethyl-4H-[1,3]dioxino[4,5-c]pyridine dichloride (10a) which demonstrated lower MIC values against S. aureus and S. epidermidis (1 μg/ml) and lower cytotoxicity on HEK-293 cells (CC50 = 200 μg/ml). Compound 10a had no significant mutagenic and genotoxic effects and was selected for further evaluation. It should be noted that all bis-phosphonium salt based on pyridoxine were much more toxic than vancomycin. 相似文献
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Shtyrlin VG Zyavkina YI Ilakin VS Garipov RR Zakharov AV 《Journal of inorganic biochemistry》2005,99(6):1335-1346
Formation constants and structures of copper(II) complexes with oxidized glutathione (L) have been determined by computer modelling of spectrophotometric and NMR relaxation measurements data over a wide range of pH (1-13) and metal and ligand concentrations in aqueous KNO(3) (1M) at 298K. Among 11 found complexes, four forms were characterized for the first time. Based on a comparison of thermodynamic, relaxation, and optical and EPR spectroscopy parameters the structural conclusions were made. In particular, the CuLH(2) and CuLH(-) complexes both contain two isomers which are similar to mono- and bis-aminoacid copper(II) complexes. In the Cu(2)L and Cu(3)L(2)(2-) species one of the copper atoms is bound only with the carboxylate or carbonyl groups and the others are coordinated similarly to aminoacid chelates. Along with the last, in Cu(2)LH(-2)(2-) two bridging OH(-) groups in one isomer or two chelate rings including deprotonated peptide nitrogen and glycinyl carboxylate oxygen in another are also present. In Cu(3)L(2)H(-4)(6-) the mixed variant of coordination between CuL(2-) (CuN(2)O(2)) and Cu(2)LH(-4)(4-)(CuN(3)O) is realized. The structures of polynuclear complexes have been optimized in density functional theory computations. Rate constants of ligand exchange reactions of Cu(LH)(2)(4-) and CuL(2)(6-) with participation of the LH(3-) and L(4-) forms were determined for the first time. Factors determining rates of these processes have been revealed and their proceeding by associative substitution mechanism shown. 相似文献
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Felix D. Sokolov Valery G. Shtyrlin Vasily V. Brusko Sergey V. Baranov Tadeusz Glowiak 《Inorganica chimica acta》2006,359(7):2087-2096
Thiourea, PhNHC(S)NHP(O)(OPri)2 (LH) chelates of CoII, NiII, and PdII ions have been obtained and investigated by single-crystal X-ray diffraction, UV, IR, NMR spectroscopy, and EI mass-spectrometry. The unusual 1,3-N,S-coordination via sulfur and NP(O) nitrogen atoms has been found in the trans-square-planar NiL2 and PdL2 complexes, whereas the 1,5-O,S-coordination is realized in the tetrahedral CoL2 complex. DFT calculations have revealed significant stabilization of the 1,3-N,S-structures due to stronger crystal field and the NH-OP hydrogen bonds. 相似文献
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Roman S. Pavelyev Oksana V. Bondar Thi N.T. Nguyen Alisa A. Ziganshina Mohammad Al Farroukh Rawdah Karwt Gulnaz D. Alekbaeva Mikhail V. Pugachev Zilya R. Yamaleeva Olga N. Kataeva Konstantin V. Balakin Yurii G. Shtyrlin 《Bioorganic & medicinal chemistry》2018,26(22):5824-5837
Two series of novel pyridoxine-based azaheterocyclic analogs of feruloyl methane (Dehydrozingerone, DZG) were synthesized, and their biological activity against a panel of tumor and normal cell lines was evaluated in vitro. The most active compounds possessed expressed cytotoxic activity, which was comparable to cytotoxic activity of doxorubicin and significantly higher than that of DZG, and a remarkable selectivity for the studied cancer cell lines as compared to the normal cells. The leading compound and DZG initiated arrest of the cell cycle in the G2/M phase, preventing normal division and further transition of daughter cells to the G0/G1 phase. Similar to DZG, but with higher efficiency, the leading compound was able to inhibit migration activity and, therefore, invasiveness of tumor cells. It also increased concentration of reactive oxygen species in tumor cells, induced depolarization of mitochondrial membranes and initiated apoptosis accompanied by disruption of integrity of cytoplasmic cell membranes. By contrast to DZG, the leading compound did not possess antioxidant properties. The obtained data make the described chemotype a promising starting point for the development of new anticancer agents. 相似文献
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