Репозиторий Университета

© 2018, © 2018 Taylor  &  Francis. A library of 29 2-amino-6-sulfanylpyridine-3,5-dicarbonitriles functionalized with a pyridoxine moiety was synthesized using a three-component one-pot reaction of aldehyde derivative of pyridoxine, malononitrile, and thiophenol. The obtained bipyridine structures were converted into methylpyridinium salts. Several compounds demonstrated expressed antibacterial activity with MICs (minimum inhibitory concentrations) in the range of 0.5–4 µg/mL against the three studied Gram-positive strains and 8–64 µg/mL against the Gram-negative E. coli strain, which was comparable or better than the activity of the reference antimicrobial agents. At the same time, all the synthesized compounds were inactive against the Gram-negative P. aeruginosa. Several compounds also demonstrated high cytotoxic activity against the studied tumor cells, but without selectivity for the normal HSF (human foreskin fibroblast) cells. Despite the preliminary character of the performed biological studies, the obtained results make the obtained structural chemotype a promising starting point for the design of physiologically active compounds.

© 2018 Wolters Kluwer Health, Inc. All rights reserved. This work presents the results of in-vitro biological activity studies of three novel anticancer agents, phosphonium salts based on the 3-hydroxypyridine scaffold, including one derivative of 4-deoxypyridoxine. Proliferation and viability of cells treated with these compounds was assessed by the colony formation and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays. Effects of the compounds on apoptosis and cell cycle were studied by flow cytometry using annexin V-FITC/propidium iodide and propidium iodide staining, respectively. The influence of the compounds on mitochondrial membrane potential and intracellular reactive oxygen species was evaluated using tetramethyl rhodamine ethyl and DCFHA staining. Western blot analysis was used to study the changes in the expression of Bcl-xL, Bax, and caspase-3 apoptotic proteins. The treatment of ovarian adenocarcinoma cells OVCAR-4 with the tested compounds inhibited the growth and induced cell cycle arrest in the G1 phase. 3-Hydroxypyridine derivatives induced apoptosis by hyperexpression of Bax and caspase-3, whereas 4-deoxypyridoxine derivative induced cell death partly by reactive oxygen species generation and caspase-3 hyperexpression. These results indicate that the quaternary phosphonium salts studied represent potential therapeutic agents for the treatment of ovarian cancer.

© 2018, Copyright © Kazan (Volga region) Federal University. The syntheses of a series of novel derivatives of stilbazole and their azo-analogs bearing the phenylalkenyl and phenyldiazenyl substituents at position 6 of the pyridoxine ring are reported. The observed cis/trans regioselectivity in the Wittig reaction between triphenylbenzylphosphonium chloride and carbonyl derivatives of pyridoxine ketal is discussed with respect to transition state intermediates, nature of base used in the reaction, and resonance transformations in the pyridoxine system. The azo-derivatives are obtained by azocoupling of the diazonium salts of sulfanilic or 4-aminophenyl-1,3-disulfonic acids with the corresponding pyridoxine acetals. Nine compounds from the obtained experimental series are capable of emitting second harmonic generation light, although with a reduced efficiency as compared to well known KH2PO4 or LiIO3 perovskite crystals, but with excellent beam resistance under laser irradiation, which makes them potential starting points for the development of novel nonlinear optical materials.

© 2018 Ima-Press Publishing House. All Rights Reserved. Information about a favorable prognosis for a patient, recommendations for activities, and optimal pharmacotherapy are a mainstay in the effective treatment of acute nonspecific low back pain (NLBP). Standard pharmacotherapy for acute NLBP includes nonsteroidal anti-inflam-matory drugs (NSAIDs). However, the longer their administration and larger doses, the higher the risk of side effects are. NSAIDs are contraindicated in some cases. In this connection, it has become necessary to search for new opportunities for the pharmacotherapy of acute NLBP. The results of experimental studies have demonstrated the analgesic and anti-inflammatory effects of high-dose B vitamins. Clinical trials have confirmed the efficacy of Vitamin B complex (thiamine, pyridoxine, and cyanocoba lamin) in the treatment of acute NLBP. The paper considers the practical significance of concomitant administration ofB vitamins and NSAIDs in NLBP and notes the efficacy of milgamma used both alone and in combination with NSAIDs in the treatment of acute NLBP.