Galanthamine Chemistry. VII. Synthesis of Analogues of Galanthamine

Polymorphic Study of (-)-galanthamine Hydrobromide

Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution.

(-)-Galanthamine (GAL), an alkaloid from the flower, the common snowdrop (Galanthus nivalis), shows anticholinesterase activity. This property has made GAL the target of research as to its effectiveness in the treatment of Alzheimer's disease. We have solved the X-ray crystal structure of GAL bound in the active site of Torpedo californica acetylcholinesterase (TcAChE) to 2.3 A resolution. The ...

Synthesis of Precursors for the Oxidative Tandem Cyclization of Diphenols to Galanthamine Analogs

Methods for the preparation of 4-bromo-5-[2-(4-hydroxybenzyl)benzyl]-2methoxyphenol and 4-bromo-5-[4-(4-hydroxyphenyl)butyl]-2-methoxyphenol are described.

Nivalin (galanthamine hydrobromide), an additional decurarizing agent. Some introductory observations.

Galanthamine hydrobromide (Nivalin), an alkaloid from the bulbs of snowdrops, is widely used in Bulgaria as an antagonist to non-depolarizing muscle relaxants. The pharmacology is reviewed and experiences in the use of galanthamine in 24 patients are described. It is about one-tenth as potent as neostigmine. As changes in pulse rate and blood pressure were slight, it is rarely necessary to inje...

Synthesis and evaluation of (-)- and (+)-[¹¹C]galanthamine as PET tracers for cerebral acetylcholinesterase imaging.

Improved radiopharmaceuticals for imaging cerebral acetylcholinesterase (AChE) are needed for the diagnosis of Alzheimer's disease (AD). Thus, (11)C-labeled (-)-galanthamine and its enantiomers were synthesized as novel agents for imaging the localization and activity of AChE by positron emission tomography (PET). C-11 was incorporated into (-)- and (+)-[(11)C]galanthamine by N-methylation of n...