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

Pelayo Camps, D. Munoz-Torrero

Open publisher page 40 citations

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

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What this paper is about

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

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Available 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

Key concepts: Tacrine, Huperzine A, Acetylcholinesterase, Aché, Chemistry, Acetylcholinesterase inhibitor, Pharmacology, Enzyme

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