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■ Synthesis and Anti-Acetylcholinesterase Activity of Thiaphysostigmine Derivatives

Masayuki An-naka, Kosuke Yasuda, Masaki Yamada, Akiyosi Kawai, Norio Takamura,* Shigehiko Sugasawa (the late), Yuzo Matsuoka, Hirosi Iwata, and Tomiko Fukushima

*Organic Chemistry Research Laboratory, Tanabe Seiyaku Co.Ltd., 2-2-50, Kawagishi, Toddda, Saitama 335-8505, Japan

Abstract

A series of thiaphysostigmine derivatives (2a, b and 3a, b), with a sulfur atom instead of N-methyl group in B ring or C ring of physostigmine (1), were synthesized, and their inhibitory effects on AChE and BuChE activity, and acute toxicity were evaluated.