- Synthesis and in vitro evaluation of galanthamine derivatives for examination of nicotinic acetylcholine receptor system
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The synthesis and radioactive labeling of several galanthamine derivatives, 6-O-demethyl-6-O-fluoroethylgalanthamine, 10-N-demethyl-10-N-fluoroethylgalanthamine and N-methylgalanthaminium are reported. First in vitro evaluation were carried out to determine their properties as allosterically potentiating ligands of nicotinic receptors. N-methylgalanthaminium was found to be a promising candidate for further investigations.
- Schildan, A.,Schirrmacher, R.,Samochocki, M.,Christner, C.,Mmaelicke, A.,Roesch, F.
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- ALKALOID N-OXIDES FROM LYCORIS SANGUINEA
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Three new alkaloids, galanthamine N-oxide, sanguinine N-oxide and lycoramine N-oxide were isolated from Lycoris sanguinea var.Kiushiana Makino.
- Kobayashi, Shigeru,Satoh, Kimihito,Numata, Atsushi,Shingu, Tetsuro,Kihara, Masaru
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- Synthesis and structure-activity relationships of open D-Ring galanthamine analogues
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Open D-ring galanthamine analogues were prepared using ring-opening reactions of the quaternarized urethane or oxazolidine functions and were evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition potency.
- Herlem, Denyse,Martin, Marie-Therese,Thal, Claude,Guillou, Catherine
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- METHOD FOR THE PRODUCTION OF HIGH-PURITY 4A, 5, 9, 10, 11, 12,-HEXAHYDRO-6H-BENZOFURO [3A, 3, 2-EF] [2] BENZAZEPINE, AND THE DERIVATIVES THEREOF
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A process for the production of extremely pure galanthamine or extremely pure galanthamine derivatives, whereby a start is made from racemic bromine narwedine, which is debrominated under palladium catalysis. The working-up of the reaction mixture, which is carried out in the presence of oxygen or peroxides, is essential to the process, so that the palladium catalyst is converted into an insoluble form, a form that can be easily separated. The further reaction is carried out by reduction of enantiomerically pure narwedine to form enantiomerically pure galanthamine, whereby it is then alkylated or dealkylated, so that a corresponding substitution on the ring-nitrogen atom is achieved. By further purification, such as recrystallization, residual portions of palladium of below 5 ppm are achieved, so that the direct use as a pharmaceutical raw material is made possible.
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(2010/05/13)
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