- The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca2+/calmodulin-dependent kinase II
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An affinity capillary electrophoresis (ACE) method to estimate apparent dissociation constants between bovine brain calmodulin (CaM) and non-peptidic ligands was developed. The method was validated reproducing the dissociation constants of a number of wel
- Bruno, Claudio,Cavalluzzi, Maria Maddalena,Rusciano, Maria Rosaria,Lovece, Angelo,Carrieri, Antonio,Pracella, Riccardo,Giannuzzi, Giulia,Polimeno, Lorenzo,Viale, Maurizio,Illario, Maddalena,Franchini, Carlo,Lentini, Giovanni
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supporting information
p. 36 - 45
(2016/04/19)
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- A convenient synthesis of lubeluzole and its enantiomer: Evaluation as chemosensitizing agents on human ovarian adenocarcinoma and lung carcinoma cells
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Lubeluzole, a neuroprotective anti-ischemic drug, and its enantiomer were prepared following a convenient procedure based on hydrolytic kinetic resolution. The ee values were >99% and 96%, respectively, as assessed by HPLC analysis. The chemosensitizing e
- Cavalluzzi, Maria Maddalena,Viale, Maurizio,Bruno, Claudio,Carocci, Alessia,Catalano, Alessia,Carrieri, Antonio,Franchini, Carlo,Lentini, Giovanni
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p. 4820 - 4823
(2013/09/02)
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- Synthesis of N-methyl secondary amines
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A diverse set of N-methyl secondary amines are obtained in high yields by an expedient reductive alkylation of commercially available methanolic methylamine.
- Kumpaty, Hephzibah J.,Williamson, John S.,Bhattacharyya, Sukanta
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p. 1411 - 1416
(2007/10/03)
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- Facile preparation of N-methyl secondary amines by titanium(IV) isopropoxide-mediated reductive animation of carbonyl compounds
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A simple, mild and efficient procedure for obtaining N-methyl secondary amines from aldehydes and ketones is reported. Treatment of carbonyl compounds with methylamine hydrochloride, triethylamine and titanium(IV) isopropoxide, followed by in situ sodium borohydride reduction and straightforward aqueous work-up, affords clean products in good to excellent yields.
- Neidigh, Kurt A.,Avery, Mitchell A.,Williamson, John S.,Bhattacharyya, Sukanta
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p. 2527 - 2531
(2007/10/03)
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- New antihistaminic N-heterocyclic 4-piperidinamines. 1. Synthesis and antihistaminic activity of N-(4-piperidinyl)-1H-benzimidazol-2-amines
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The synthesis of a series N-(4-piperidinyl)-1H-benzimidazol-2-amines and the preliminary evaluation of their in vitro and in vivo antihistaminic activity are described. Cyclodesulfurization of (2-aminophenyl) thioureas with mercury(II) oxide resulted in 2-aminobenzimidazole intermediates, which were monoalkylated on the endo-nitrogen atom. After deprotection of the piperideine nitrogen atom with 48% aqueous hydrobromic acid solution, the title compounds were obtained by three different methods, viz. alkylation, reductive amination, or oxirane ring-opening reactions. The in vivo antihistaminic activity was evaluated by the compound 48/80 induced lethality test in rats and histamine-induced lethality test in guinea pigs after oral and/or subcutaneous administration. The duration of action, for a selected number of compounds, was studied in the guinea pig. The phenylethyl derivatives showed the most potent antihistamine properties after oral administration in both animal species.
- Janssens,Torremans,Janssen,Stokbroekx,Luyckx
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p. 1925 - 1933
(2007/10/02)
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- N-Heterocyclyl-4-piperidinamines
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Novel N-heterocyclyl-4-piperidinamines wherein said heterocyclic radical is an optionally substituted 1H-benzimidazol-2-yl or 3H-imidazo[4,5-b]pyridin-2-yl radical, said compounds being useful as antihistaminic agents.
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