Regarding Alzheimer's disease (AD), which is characterized by progressive loss of memory and impairment in cognition, is becoming a serious threat to life expectancy especially for the elderly, and current clinical therapy is mainly palliative treatment targeting acetylcholinesterase (AChE), this study focused to screening potential ffavonoids for treatment of AD. Chalcone and aurone derivatives were synthesized and tested in vitro for AChE inhibitory activity, that yielded 8 chalcones (C1-C8) and 8 corresponding aurones (A1-A8). By biological tests, in general, the aurones showed better AChE inhibitory activity than the corresponding chalcones (at the same concentration); of them, the most potent was Auron A8 (3', 4', 5'-trimethoxyaurone). The methoxy group either in 3' or 5' position in Bring of aurones seemed to be an important moiety for binding to active sites, which resulted in an increase in AChE inhibitory capacity.
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