@article {205, title = {Tacrine-based dual binding site acetylcholinesterase inhibitors as potential disease-modifying anti-Alzheimer drug candidates}, journal = {Chemico-biological interactions}, year = {2010}, month = {2010/02/16/}, abstract = {Two novel families of dual binding site acetylcholinesterase (AChE) inhibitors have been developed, consisting of a tacrine or 6-chlorotacrine unit as the active site interacting moiety, either the 5,6-dimethoxy-2-[(4-piperidinyl)methyl]-1-indanone fragment of donepezil (or the indane derivative thereof) or a 5-phenylpyrano[3,2-c]quinoline system, reminiscent to the tryciclic core of propidium, as the peripheral site interacting unit, and a linker of suitable length as to allow the simultaneous binding at both sites. These hybrid compounds are all potent and selective inhibitors of human AChE, and more interestingly, are able to interfere in vitro both formation and aggregation of the beta-amyloid peptide, the latter effects endowing these compounds with the potential to modify Alzheimer{\textquoteright}s disease progression.}, author = {Camps,P. and Formosa,X. and Galdeano,C. and Gomez,T. and Munoz-Torrero,D. and Ramirez,L. and Viayna,E. and Gomez,E. and Isambert,N. and Lavilla,R. and Badia,A. and Clos,M. V. and Bartolini,M. and Mancini,F. and Andrisano,V. and A. Bidon-Chanal and Huertas,O. and Dafni,T. and F. J. Luque} }