Chemical and Pharmaceutical Bulletin p. 529 - 538 (1993)
Update date:2022-08-04
Topics:
Ishihara
Miyamoto
Nakayama
Goto
Inhibitors of acetylcholinesterase (AChE) bave been designed based on a working hypothesis of the enzyme's active site. These compounds were tested for their inhibitory activities on AChE and ω-[N-ethyl-N-(phenylmethyl)amino]-1-phenyl-1-alkanones (3) were found to be potent inhibitors. Various analogues of 3 were prepared to study the effect on AChE inhibition of partial restriction of conformation. Compounds with potent AChE inhibition were further evaluated in terms of central selectivity: the ratio of central action (ameliorating effect on scopolamine-induced memory impairment using a T-maze alternation task) to peripheral action.
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