132219-07-9Relevant academic research and scientific papers
Central cholinergic agents. IV. Synthesis and acetylcholinesterase inhibitory activities of ω-[N-ethyl-N-(phenylmethyl)amino]-1-phenyl-1-alkanones and their analogues with partial conformational restriction
Ishihara,Miyamoto,Nakayama,Goto
, p. 529 - 538 (2007/10/02)
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.
