- Use of nitrogen-containing heterocyclic radical substituted alkene compounds
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The invention relates to new use of a series of nitrogen-containing heterocyclic radical substituted alkene compounds, and more specifically relates to use of the compounds represented by general formula a or salts thereof in bioimaging, pH value detection, biomacromolecule detection or cell microenvironment detection, wherein Z, S1, S2 and R1 are defined as the specification. The compounds are utilized as the fluorescent dye for bioimaging, fluorescent pH probe for pH value detection and/or diagnostic agent for tumor cell detection. The compounds involved in the invention have excellent imaging effect, and shows the single component multicolor property, can be used for single component multicolor imaging or conventional imaging, etc., and haves enormous application prospect in bioimaging and tumor detection. (formula a).
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Paragraph 0292-0294
(2017/09/12)
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- Metal-free oxidative olefination of primary amines with benzylic C-H bonds through direct deamination and C-H bond activation
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An oxidative olefination reaction between aliphatic primary amines and benzylic sp3 C-H bonds has been achieved using N-bromosuccinimide as catalyst and tert-butyl hydroperoxide as oxidant. The olefination proceeds under mild metal-free conditions through direct deamination and benzylic C-H bond activation, and provides easy access to biologically active 2-styrylquinolines with (E)-configuration. This journal is the Partner Organisations 2014.
- Gong, Liang,Xing, Li-Juan,Xu, Tong,Zhu, Xue-Ping,Zhou, Wen,Kang, Ning,Wang, Bin
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supporting information
p. 6557 - 6560
(2014/08/18)
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- Microwave-assisted solvent-free synthesis of 2-styrylquinolines in the presence of zinc chloride
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An efficient solvent-free procedure has been developed for the synthesis of (E)-2-styrylquinoline derivatives under microwave irradiation in the presence of zinc chloride. The developed procedure is advantageous due to shorter reaction time and simpler wo
- Li,Gavrishova,Budyka
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p. 823 - 828
(2012/11/13)
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- Synthesis of hydroxystyrylquinolines and hydroxystyryl-2,2′- bipyridine under uncatalyzed and solvent-free conditions using microwave irradiation
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The possibility was explored of synthesizing trans-isomers of 2-(4-hydroxystyryl)quinoline, 2-(4-hydroxystyryl)-7-chloroquinoline, 3-(4-hydroxystyryl)benzo[f]quinoline, and 6-(4-hydroxystyryl)-2,2′- bipyridine under uncatalyzed and solvent-free conditions
- Gavrishova,Lee,Gor'Kov,Budyka
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experimental part
p. 507 - 509
(2011/08/02)
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- Synthesis, spectral and photochemical properties of the styrylquinoline-naphthol dyad with a dioxytetramethylene bridge
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The luminescence of 2-naphthol and 2-styrylquinoline fragments, intramolecular energy transfer from the former to the latter, and photoisomerization of the latter are observed in the newly synthesized bichromophoric dyad.
- Budyka, Mikhail F.,Sadykova, Kristina F.,Gavrishova, Tatyana N.
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experimental part
p. 151 - 152
(2011/12/02)
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- Synthesis of photoactive bichromophoric dyads containing 2-styrylquinoline and 2-naphthol moieties
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A three-step approach to the synthesis of bichromophoric dyads of the general formula SQ - (CH2)n - Np (SQ is the 2-(4-oxystyryl)quinoline moiety, Np is the 3-oxy-2-naphthol moiety, n = 2, 4, 5) was developed from available reagents.
- Gavrishova,Li,Sadykova,Budyka
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experimental part
p. 1495 - 1499
(2012/07/13)
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- Development of a novel series of styrylquinoline compounds as high- affinity leukotriene D4 receptor antagonists: Synthetic and structure- activity studies leading to the discovery of (±)-3-[[[3-[2-(7-chloro-2- quinolinyl)-(E)-ethenyl]phenyl][[3-(dimethylamino)-3- oxopropyl]thio]methyl]thio]propionic acid
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Based on LTD4 receptor antagonist activity of 3-(2-quinolinyl-(E)- ethenyl)pyridine (2) found in broad screening, structure-activity studies were carried out which led to the identification of 3-[[[3-[2-(7-chloro-2- quinolinyl)-(E)-ethenyl]phenyl][[3-(dimethylamino)-3- oxopropyl]thio]methyl]thio]propionic acid (1, MK-571) as a potent and orally active LTD4 receptor antagonist. These studies demonstrated that a phenyl ring could replace the pyridine in 2 without loss of activity, that 7-halogen substitution in the quinoline group was optimal for binding, that the (E)- ethenyl linkage was optimal, that binding was enhanced by incorporation of a polar acidic group or groups in the 3-position of the aryl ring, and that two acidic groups could be incorporated via a dithioacetal formed from thiopropionic acid and the corresponding styrylquinoline 3-aldehyde to yield compounds such as 20 (IC50 = 3 nM vs [3H]LTD4 binding to the guinea pig lung membrane). It was found that one of the acidic groups could be transformed into a variety of the amides without loss of potency and that the dimethylamide 1 embodied the optimal properties of intrinsic potency (IC50 = 0.8 nM on guinea pig lung LTD4 receptor) and oral in vivo potency in the guinea pig, hyperreactive rat, and squirrel monkey. The evolution of 2 to 1 involves the increase of >6000-fold in competition for [3H]LTD4 binding to guinea pig lung membrane and a >40-fold increase in oral activity as measured by inhibition of antigen-induced dyspnea in hyperreactive rats.
- Zamboni,Belley,Champion,Charette,DeHaven,Frenette,Gauthier,Jones,Leger,Masson,McFarlane,Metters,Pong,Piechuta,Rokach,Therien,Williams,Young
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p. 3832 - 3844
(2007/10/02)
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- QUINOLINE DERIVATIVES AND USE THEREOF AS ANTAGONISTS OF LEUKOTRIENE D4
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This invention relates to quinolinyl compounds of the general formula: STR1 and the use of these compounds as pharmacological agents which are lipoxygenase inhibitors and/or leukotriene antagonists possessing anti-inflammatory and anti-allergic properties
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