Central cholinergic agents. IV. Synthesis and acetylcholinesterase inhibitory activities of omega-[N-ethyl-N-(phenylmethyl)amino]-1-phenyl-1-alkanones and their analogues with partial conformational restriction.
- Published Article
Chemical & pharmaceutical bulletin
- Publication Date
Mar 01, 1993
Inhibitors of acetylcholinesterase (AChE) have been designed based on a working hypothesis of the enzyme's active site. These compounds were tested for their inhibitory activities on AChE and omega-[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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The corresponding record at NLM can be accessed at https://www.ncbi.nlm.nih.gov/pubmed/8477504