- Synthesis and photophysical properties of fluorescent arylstyrylimidazo[1,2-a]pyridine-based donor-acceptor chromophores
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A series of novel fluorescent arylstyrylimidazo[1,2-a]pyridines was synthesized and fully characterized. All styryl derivatives have an E-configuration of the vinyl double bond as unequivocally shown by 1H NMR spectroscopy. It was observed that
- Sefero?lu, Zeynel,Ihmels, Heiko,?ahin, Ertan
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p. 465 - 473
(2015/03/18)
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- General and selective reductive amination of carbonyl compounds using a core-shell structured Co3O4/NGr@C catalyst
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The application of heterogenized non-noble metal-based catalysts in selective catalytic hydrogenation processes is still challenging. In this respect, the preparation of a well-defined cobalt-based catalyst was investigated by immobilization of the corresponding cobalt(ii)-phenanthroline-chelate on Vulcan XC72R carbon powder. The formed core-shell structured cobalt/cobalt oxide nanocomposites are encapsulated by nitrogen-enriched graphene layers. This promising cheap heterogeneous catalyst allows for an efficient domino reductive amination of carbonyl compounds with nitroarenes. This journal is
- Stemmler, Tobias,Westerhaus, Felix A.,Surkus, Annette-Enrica,Pohl, Marga-Martina,Junge, Kathrin,Beller, Matthias
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p. 4535 - 4540
(2014/12/10)
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- Iron-catalyzed synthesis of secondary amines: On the way to green reductive aminations
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Amines represent important intermediates in chemical and biological processes. Herein, we describe the use of a nanostructured iron-based catalyst for the tandem reductive amination between nitroarenes and aldehydes using hydrogen as reductant. The nanostructured iron-catalyst is prepared by immobilization of an iron-phenanthroline complex onto a commercially available carbon support. In the reaction sequence a primary amine is formed in situ from the corresponding nitro compound. Reversible condensation with aldehydes forms the respective imines, which are finally reduced to the desired secondary amine. This synthesis of secondary amines is atom-economical and environmentally attractive using cheap and readily available organic compounds as starting materials.
- Stemmler, Tobias,Surkus, Annette-Enrika,Pohl, Marga-Martina,Junge, Kathrin,Beller, Matthias
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p. 3012 - 3016
(2015/09/28)
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- Analogue-based design, synthesis and docking of non-steroidal anti-inflammatory agents. Part 2: Methyl sulfanyl/methyl sulfonyl substituted 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-ones
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A series of methyl sulfanyl/methyl sufonyl substituted 2,3-diaryl-2,3- dihydro-1H-quinazolin-4-one were designed using analogue-based design, scaffold hopping and shape similarity matching. The designed compounds were synthesized in 2-3 steps with simple chemistry and screened by ovine cyclooxygenases (COXs) inhibitory assay and carrageenan-induced rat paw edema assay. Among the screened compounds, two compounds exhibited 100% cyclooxygenase-2 (COX-2) inhibitory potency without showing cycloxygenase-1 (COX-1) inhibition at 20 μM. The compounds also showed promising in vivo anti-inflammatory potential. A structure-activity relationship within the dataset was established by correlating the effect of aromatic ring substituent constants, structural variables and physico-chemical descriptors with in vivo anti-inflammatory activity. Molecular docking studies were also performed on the title compounds to study the binding interactions to COX-2 active site residues. The experimentally determined COX-2 inhibitory activity was found moderately correlating with binding modes predicted for compounds by Glide XP dock scoring function. The 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-one pharmacophore reported herein should be a new lead for further development of novel non-steroidal anti-inflammatory agents.
- Manivannan,Chaturvedi
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p. 7119 - 7127
(2013/01/15)
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- 1,5-Diarylimidazoles with strong inhibitory activity against COX-2 catalyzed PGE2 production from LPS-induced RAW 264.7 cells
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A series of 1,5-diarylimidazoles with 4-methylsulfonylphenyl group were prepared and evaluated for the inhibitory activities against COX-2 catalyzed PGE2 production from LPS-induced RAW 264.7 cells. Most of synthesized 1,5-diarylimidazoles exhibited strong inhibitory activities regardless of the position of the 4-methylsulfonylphenyl group. The 1,5-diarylimidazoles with a halogen atom (3c-3h, 3n-3p) gave mostly excellent inhibitory activities regardless of the position and species of the halogen atom. Whereas the 1,5-diarylimidazoles with two fluorine atoms (3k, 3l, 3r, 3s) showed rather reduced inhibitory activities.
- Che, Haiyan,Tuyen, Truong Ngoc,Kim, Hyun Pyo,Park, Haeil
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p. 4035 - 4037
(2010/08/06)
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