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Synthesis and cholinesterase inhibitory activity of 6-, 7-methoxy-(and hydroxy-) tacrine derivatives.

Maria Rosaria Del Giudice, Anna Borioni, Carlo Mustazza, F. GATTA, Annarita Meneguz, Maria Teresa Volpe

Abstract

Some 6- and 7-methoxy-(and hydroxy-) tacrine derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities. The most potent analogue in our series was the 9-heptylamino-6-methoxytacrine 3af which, in comparison with tacrine (THA), displayed an almost identical inhibitory effect, slightly lower acute toxicity and higher selectivity profile towards AchE when compared with THA.

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Key concepts: Tacrine, Butyrylcholinesterase, Acetylcholinesterase, Chemistry, Cholinesterase, Aché, Enzyme inhibitor, Inhibitory postsynaptic potential