title: Highly selective inhibition of butyrylcholinesterase by a novel melatonin-tacrine heterodimers.
abstract: Novel inhibitors of cholinesterases, especially butyrylcholinesterase (BuChE), were obtained by coupling melatonin-tacrine heterodimers via the carbamate bond. Compounds 14a-i possessed potent cholinesterase inhibitory activity (with IC50 values as low as 1.18 nM for acetylcholinesterase (AChE) and 0.24 nM for butyrylcholinesterase (BuChE)). These heterodimers exhibit selectivity toward BuChE, being from 4- to 256-fold more active toward BuChE than AChE, but still acting as better AChE inhibitors than tacrine 4.
authors: Faculty of Chemistry, University of Warsaw, Warsaw, Poland.
authors: Anna
authors: A
authors: Zawadzka
authors: Iwona
authors: I
authors: Lozińska
authors: Zuzanna
authors: Z
authors: Molęda
authors: Mirosława
authors: M
authors: Panasiewicz
authors: Zbigniew
authors: Z
authors: Czarnocki
mesh_terms: D002091:Butyrylcholinesterase / Q000187:drug effects*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D008550:Melatonin / Q000494:pharmacology*; D013619:Tacrine / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D002800:Cholinesterase Inhibitors; D013619:Tacrine; D002091:Butyrylcholinesterase; D008550:Melatonin
keywords: Alzheimer's disease; cholinesterases inhibitors; hybrid drugs