1991•Bioorganic & Medicinal Chemistry LettersOpen access

Synthesis and biological activity of galanthamine derivatives as acetylcholinesterase (AChE) inhibitors

So‐Yeop Han, Scott C. Mayer, Edwin J. Schweiger, Bonnie M. Davis, Madeleine M. Joulleé

Abstract

The syntheses of several ester and carbamate derivatives of galanthamine are described. These compounds are potential therapeutic agents in the treatment of Alzheimer's disease (AD). The inhibition of cortical acetylcholinesterase (AChE) by these drug candidates with different side chains was investigated. Side chain length as well as branching affected the AChE inhibitory activity. Esters were generally less effective than carbamates.

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Key concepts: Acetylcholinesterase, Chemistry, Carbamate, Aché, Stereochemistry, Biological activity, Enzyme inhibitor, Enzyme