Tacrine-Huperzine A Hybrids (Huprines) A New Class of Highly Potent and Selective Acetylcholinesterase Inhibitors of Interest for the Treatment of Alzheimer Disease

Authors: Camps P.; Munoz-Torrero D.

Source: Mini Reviews in Medicinal Chemistry, Volume 1, Number 2, July 2001 , pp. 163-174(12)

Publisher: Bentham Science Publishers

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Abstract:

Tacrine-huperzine A hybrids (huprines) are a new class of very potent and selective acetylcholinesterase (AChE) inhibitors. Huprines were designed from tacrine and (-)-huperzine A through a conjunctive approach. They combine the 4-aminoquinoline substructure of tacrine with the carbobicyclic substructure of (-)-huperzine A. Structural variations on several parts of a lead structure have allowed to complete a structure-activity relationship exploration of this new structural family and have led to several huprines more active than other known AChE inhibitors.

Keywords: Tacrine-huperzine A hybrids (huprines); acetylcholinesterase (AChE) inhibitors; tacrine; (-)-huperzine A; amyloid peptide; amyloid precursor proteine; Acetylcholinesterase; Torpedo Californica Acetylcholinesterase

Language: English

Document Type: Review article

DOI: 10.2174/1389557013406972

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