Rational design of central selective acetylcholinesterase inhibitors by means of a “bio-oxidisable prodrug” strategy

…, N Le Fur, G Hagues, J Costentin, N Torquet…

文献索引：Bohn, Pierre; Le Fur, Nicolas; Hagues, Guillaume; Costentin, Jean; Torquet, Nicolas; Papamicael, Cyril; Marsais, Francis; Levacher, Vincent Organic and Biomolecular Chemistry, 2009 , vol. 7, # 12 p. 2612 - 2618

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被引用次数: 12

摘要

This work deals with the design of a “bio-oxidisable prodrug” strategy for the development of new central selective acetylcholinesterase inhibitors. This prodrug approach is expected to reduce peripheral anticholinesterase activity responsible for various side effects observed with presently marketed AChE inhibitors. The design of these new AChE inhibitors in quinoline series is roughly based on cyclic analogues of rivastigmine. The key activation ...