Resveratrol Derived Butyrylcholinesterase Inhibitors

Novel polyhydroxylated (E)‐stilbenes were synthesized by Mizoroki–Heck reactions and tested for their ability to inhibit the enzymes acetyl‐ and butyrylcholinesterase. Several of them are good inhibitors of butyrylcholinesterase; one of them carrying an extra fluorine substituent is a 94‐fold strong...

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Veröffentlicht in:	Archiv der Pharmazie (Weinheim) 2013-07, Vol.346 (7), p.499-503
Hauptverfasser:	Csuk, René, Albert, Sabrina, Kluge, Ralph, Ströhl, Dieter
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholinesterase Acetylcholinesterase - metabolism Alzheimer disease Butyrylcholinesterase Butyrylcholinesterase - metabolism Cholinesterase Inhibitors - chemical synthesis Cholinesterase Inhibitors - pharmacology Molecular Structure Resveratrol analogs Stilbenes - chemical synthesis Stilbenes - pharmacology Structure-Activity Relationship
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Zusammenfassung:	Novel polyhydroxylated (E)‐stilbenes were synthesized by Mizoroki–Heck reactions and tested for their ability to inhibit the enzymes acetyl‐ and butyrylcholinesterase. Several of them are good inhibitors of butyrylcholinesterase; one of them carrying an extra fluorine substituent is a 94‐fold stronger inhibitor of butyrylcholinesterase than of acetylcholinesterase. Novel polyhydroxylated (E)‐stilbenes synthesized by Mizoroki–Heck reactions were tested for their ability to inhibit the enzymes acetyl‐ and butyrylcholinesterase. Several of them were found to be good inhibitors of butyrylcholinesterase. One of them carrying an extra fluorine substituent is a 94‐fold stronger inhibitor of butyrylcholinesterase than of acetylcholinesterase.
ISSN:	0365-6233 1521-4184
DOI:	10.1002/ardp.201300051