Олег Большаков | South Ural State University (original) (raw)
Papers by Олег Большаков
5H-1,2,3-Dithiazole-5-thiones and 5H-1,2,3-dithiazol-5-ones undergo a new transformation into 1,2... more 5H-1,2,3-Dithiazole-5-thiones and 5H-1,2,3-dithiazol-5-ones undergo a new transformation into 1,2,5-thiadiazole-3(2H)-thiones
and 1,2,5-thiadiazol-3(2H)-ones, respectively, upon treatment with primary amines; the structure of thiadiazolethione was confirmed
by X-ray diffraction.
We here report the synthesis and biological evaluation of rare 4-substituted-5-phenylimino, 5-thi... more We here report the synthesis and biological evaluation of rare 4-substituted-5-phenylimino, 5-thienoand
5-oxo-1,2,3-dithiazoles. Dithiazoles were selectively obtained in moderate to high yields (25–73%)
via a one-pot reaction from various ethanoneoximes with sulfur monochloride, pyridine in acetonitrile
followed by treatment by corresponding nucleophiles (aniline, thioacetamide and formic acid). All the
synthesized compounds were screened for their antibacterial (against bacteria Escherichia coli, Salmonella
enterica serovar Typhimurium, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus,
Enterococcus faecalis, Bacillus cereus and Listeria inocua), antifungal (against pathogenic strains Candida
albicans, Candida glabrata, Candida tropicalis and Issatchenkia orientalis) and antitumor (on human cell
lines MCF-7 and MDA-MB-231) activity. 4-(2-Pyridinyl)-5H-1,2,3-dithiazole-5-thione and 4-ethylcarboxyl-
5H-1,2,3-dithiazole-5-thione (5d, 5h) that are active against Gram-positive bacteria are significantly
active against fungi. 4-(2-Benzofuranyl)-5-phenylimino-5H-1,2,3-dithiazole (4e) exerts antiproliferative
activity.
Development of biologically active polymers is an active area of research due to their applicatio... more Development of biologically active polymers is an active area of research due to their applications in varied and diverse fields of biomedical research: cell adhesion, tissue proliferation, and drug delivery. Recent advances in chemical modification allow fine-tuning of the properties of biomedical polymers to improve their applications: blood circulation half-life, stimuli-responsive degradation, site-specific targeting, drug loading, etc. In this article, convergent synthesis of polymerizable macromonomers bearing a site-specific ligand (RGD peptide) using a low molecular weight MA-poly(ethylene glycols) (PEGs) is presented. The method affords macromonomers useful as the starting materials to produce biomedical polymers. We found matrix-assisted laser desorption/ionization convenient in monitoring the conjugation process via step-by-step following of PEG modification. V C 2014 Wiley Periodicals, Inc.
5H-1,2,3-Dithiazole-5-thiones and 5H-1,2,3-dithiazol-5-ones undergo a new transformation into 1,2... more 5H-1,2,3-Dithiazole-5-thiones and 5H-1,2,3-dithiazol-5-ones undergo a new transformation into 1,2,5-thiadiazole-3(2H)-thiones
and 1,2,5-thiadiazol-3(2H)-ones, respectively, upon treatment with primary amines; the structure of thiadiazolethione was confirmed
by X-ray diffraction.
We here report the synthesis and biological evaluation of rare 4-substituted-5-phenylimino, 5-thi... more We here report the synthesis and biological evaluation of rare 4-substituted-5-phenylimino, 5-thienoand
5-oxo-1,2,3-dithiazoles. Dithiazoles were selectively obtained in moderate to high yields (25–73%)
via a one-pot reaction from various ethanoneoximes with sulfur monochloride, pyridine in acetonitrile
followed by treatment by corresponding nucleophiles (aniline, thioacetamide and formic acid). All the
synthesized compounds were screened for their antibacterial (against bacteria Escherichia coli, Salmonella
enterica serovar Typhimurium, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus,
Enterococcus faecalis, Bacillus cereus and Listeria inocua), antifungal (against pathogenic strains Candida
albicans, Candida glabrata, Candida tropicalis and Issatchenkia orientalis) and antitumor (on human cell
lines MCF-7 and MDA-MB-231) activity. 4-(2-Pyridinyl)-5H-1,2,3-dithiazole-5-thione and 4-ethylcarboxyl-
5H-1,2,3-dithiazole-5-thione (5d, 5h) that are active against Gram-positive bacteria are significantly
active against fungi. 4-(2-Benzofuranyl)-5-phenylimino-5H-1,2,3-dithiazole (4e) exerts antiproliferative
activity.
Development of biologically active polymers is an active area of research due to their applicatio... more Development of biologically active polymers is an active area of research due to their applications in varied and diverse fields of biomedical research: cell adhesion, tissue proliferation, and drug delivery. Recent advances in chemical modification allow fine-tuning of the properties of biomedical polymers to improve their applications: blood circulation half-life, stimuli-responsive degradation, site-specific targeting, drug loading, etc. In this article, convergent synthesis of polymerizable macromonomers bearing a site-specific ligand (RGD peptide) using a low molecular weight MA-poly(ethylene glycols) (PEGs) is presented. The method affords macromonomers useful as the starting materials to produce biomedical polymers. We found matrix-assisted laser desorption/ionization convenient in monitoring the conjugation process via step-by-step following of PEG modification. V C 2014 Wiley Periodicals, Inc.