TY - JOUR
T1 - Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: Subnanomolar dual binding site acetylcholinesterase inhibitors
AU - Camps, Pelayo
AU - Formosa, Xavier
AU - Muñoz-Torrero, Diego
AU - Petrignet, Julien
AU - Badia, Albert
AU - Clos, M. Victòria
PY - 2005/3/24
Y1 - 2005/3/24
N2 - 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.
AB - 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.
UR - https://www.scopus.com/pages/publications/15444378025
U2 - 10.1021/jm0496741
DO - 10.1021/jm0496741
M3 - Article
SN - 0022-2623
VL - 48
SP - 1701
EP - 1704
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 6
ER -