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
Mini-Reviews in Medicinal Chemistry
Title: Tacrine-Huperzine A Hybrids (Huprines) A New Class of Highly Potent and Selective Acetylcholinesterase Inhibitors of Interest for the Treatment of Alzheimer Disease
Volume: 1 Issue: 2
Author(s): P. Camps and D. Munoz-Torrero
Affiliation:
Keywords: Tacrine-huperzine A hybrids (huprines), acetylcholinesterase (AChE) inhibitors, tacrine, (-)-huperzine A, amyloid peptide, amyloid precursor proteine, Acetylcholinesterase, Torpedo Californica Acetylcholinesterase
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.
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Camps P. and Munoz-Torrero D., Tacrine-Huperzine A Hybrids (Huprines) A New Class of Highly Potent and Selective Acetylcholinesterase Inhibitors of Interest for the Treatment of Alzheimer Disease, Mini-Reviews in Medicinal Chemistry 2001; 1 (2) . https://dx.doi.org/10.2174/1389557013406972
DOI https://dx.doi.org/10.2174/1389557013406972 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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