Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: Subnanomolar dual binding site acetylcholinesterase inhibitors

Pelayo Camps, Xavier Formosa, Diego Muñoz-Torrero, Julien Petrignet, Albert Badia, M. Victòria Clos

Research output: Contribution to journalArticleResearchpeer-review

80 Citations (Scopus)

Abstract

A series of huprine-tacrine heterodimers has been developed by connection of huprine Y, a compound with one of the highest affinities for the active site of acetylcholinesterase yet reported, with tacrine, a compound with known affinity for the peripheral site of the enzyme, through a linker of appropriate length to allow simultaneous interaction with both binding sites. These compounds exhibit human acetylcholinesterase and butyrylcholinesterase inhibitory activities with IC50 values in the subnanomolar and low nanomolar range, respectively. © 2005 American Chemical Society.
Original languageEnglish
Pages (from-to)1701-1704
JournalJournal of Medicinal Chemistry
Volume48
Issue number6
DOIs
Publication statusPublished - 24 Mar 2005

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