Tacrine-huperzine A hybrids (huprines): a new class of highly potent and selective acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease |
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Authors: | Camps P Muñoz-Torrero D |
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Affiliation: | Laboratori de Química Farmacèutica, Facultat de Farmàcia, Universitat de Barcelona, Av Diagonal 643, E-08028, Barcelona, Spain. camps@farmacia.far.ub.es |
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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. |
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