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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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

Author(s): P. Camps and D. Munoz-Torrero

Volume 1, Issue 2, 2001

Page: [163 - 174] Pages: 12

DOI: 10.2174/1389557013406972

Price: $65

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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