Synthesis of dihydroxanthone derivatives and evaluation of their inhibitory activity against acetylcholinesterase: Unique structural analogs of tacrine based on the BCD-ring of arisugacin

A general approach to synthesis of dihydroxanthone derivatives is described here. In vitro evaluation of these dihydroxanthones demonstrated that some derivatives possess moderate anti-cholinesterase activities and better sel ectivities than tacrine for acetylcholinesterase over butyrylcholinesterase . Structural effects on anti-cholinesterase activities were also examined, and docking experiments were carried out to provide preliminary understandi ngs of these experimental observations. (C) 1999 Elsevier Science Ltd. All rights reserved.