- N,N′-bis-(3,4,5-trimethoxybenzyl) ethylenediamine N,N′-diacetic acid as a new iron chelator with potential medicinal applications against oxidative stress
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N,N′-bis-(3,4,5-trimethoxybenzyl) ethylenediamine N,N′-diacetic acid dihydrochloride (OR10141) is a member of a recently described series of "oxidative stress activatable iron chelators." These chelators have a relatively low affinity for iron but can be
- Galey, Jean-Baptiste,Dumats, Jacqueline,Genard, Sylvie,Destree, Odile,Pichaud, Patrick,Cctroux, Philippe,Marrot, Laurent,Beck, Irena,Fernandez, Bona,Barre, Gilles,Seite, Michel,Hussler, Georges,Hocquaux, Michel
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Read Online
- FBXO3 INHIBITORS
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The present application discloses benzathine and related compounds and their use as FBXO-3 inhibitors.
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Page/Page column 55
(2014/01/08)
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- Tetrahydroimidazoles - A promising group of expected NSAIDS - Their synthesis and anti-inflammatory activity
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Several new 1, 2, 3-trisubstituted tetrahydroimidazoles (11-28) have been synthesised and their structures elucidated on the basis of spectral data. These compounds show promising anti-inflammatory activity by carrageenin induced paw edema test in rats and few of them showed an activity better than indomethacin.
- Khan,Chawla, Gita
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p. 653 - 663
(2007/10/03)
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- Synthesis of novel tetrahydroimidazole derivatives and studies for their biological properties
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Ethylenediamine was reacted with suitable aromatic aldehydes in order to prepare their respective diSchiff bases. These compounds were then reduced to give the corresponding tetrahydrodiSchiff bases, which were low melting in nature. Finally, these derivatives were condensed with different aromatic aldehydes to give the desired tetrahydroimidazoles. The structures of all these compounds were established on the basis of spectral data. These novel tetrahydroimidazoles showed promising anti-inflammatory and analgesic activity. The compounds were also screened for their anti-bacterial property against Staphylococcus aureus and Escherichia coli.
- Sharma, Vibha,Khan
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p. 651 - 658
(2007/10/03)
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- O2 activation and aromatic hydroxylation performed by diiron complexes
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Chemical models of active sites of diiron oxo proteins have been synthesized. The polydendate ligands are EDTA derivatives which provide a balanced supply of nitrogen atoms and carboxylate groups together with an oxidizable phenyl moiety, thus mimicking both the iron coordination in methane monooxygenase and a nearby substrate site. All the diferric complexes have been characterized in solution by ESI-MS, optical absorption, and in some cases by 1H NMR. In the case of the ligand L1 [L1 = (N,N'-bis(3,4,5- trimethoxybenzyl)ethylenediamine N,N'-diacetic acid)], the X-ray structure of the corresponding iron complex has been determined, revealing an original tetranuclear unit, Fe4O2(L1)4·10H2O, issued from the dimerization of two [Fe2O(L1)2] units linked by carboxylate bridges. In a solution containing water or acetate, the tetranuclear complex decomposed into dinuclear complexes, which proved to be able to react with hydrogen peroxide or dioxygen in the presence of ascorbate. The final product was a mononuclear complex identified as [Fe(III)L'1(H2O)] with L'1 resulting from the quantitative hydroxylation of L1. The complex and the oxidized ligand were characterized by EPR, NMR, and UV-vis spectroscopies and by mass spectrometry. Labeling experiments showed that with both H2O2 or O2 and ascorbate, the incorporated oxygen came from the oxidant exclusively. This reaction mimicks the transformation of a tyrosine residue, brought into proximity of the active center of Ribonucleotide reductase of Escherichia coli by site-directed mutagenesis, into 3,4-dihydroxyphenylalanine.
- Ménage, Stéphane,Galey, Jean-Baptiste,Dumats, Jacqueline,Hussler, Georges,Seité, Michel,Luneau, Isabelle Gautier,Chottard, Geneviève,Fontecave, Marc
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p. 13370 - 13382
(2007/10/03)
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