Tacrine– F lurbiprofen Hybrids as Multifunctional Drug Candidates for the Treatment of Alzheimer's Disease | Zendy

Chen Yao | Zendy; Sun Jianfei | Zendy; Peng Sixun | Zendy; Liao Hong | Zendy; Zhang Yihua | Zendy; Lehmann Jochen | Zendy

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Tacrine– F lurbiprofen Hybrids as Multifunctional Drug Candidates for the Treatment of Alzheimer's Disease

Author(s) -

Chen Yao,

Sun Jianfei,

Peng Sixun,

Liao Hong,

Zhang Yihua,

Lehmann Jochen

Publication year - 2013

Publication title -

archiv der pharmazie

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.468

H-Index - 61

eISSN - 1521-4184

pISSN - 0365-6233

DOI - 10.1002/ardp.201300074

Subject(s) - tacrine , flurbiprofen , acetylcholinesterase , chemistry , butyrylcholinesterase , inhibitory postsynaptic potential , aché , pharmacology , cholinesterase , in vitro , drug , biochemistry , enzyme , medicine

Five tacrine–flurbiprofen hybrid compounds ( 3a – e ) were synthesized as multi‐target‐directed compounds for the treatment of Alzheimer's disease. Compared to tacrine, two compounds ( 3d and 3e ) showed better acetylcholinesterase (AChE) inhibitory activity and others ( 3b – e ) better or the same butyrylcholinesterase (BuChE) inhibitory activity. Notably, 3d showed a mixed‐type inhibitory action for AChE, indicating a “dual‐binding site action” of both toward the catalytic active site (CAS) and the peripheral anionic site (PAS), whereas for BuChE, a competitive inhibitory action was observed. Furthermore, a cell‐based assay on amyloid‐β inhibition demonstrated that the selected target compound 3d effectively inhibits the formation of amyloid‐β in vitro .

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