Paper
Cognition-activating properties of 3-(Aryloxy)pyridines.
Published Mar 1, 1981 · D. Butler, B. Poschel, J. Marriott
Journal of medicinal chemistry
41
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0
Influential Citations
Abstract
A series of 3-(aryloxy)pyridines was found to possess activity in enhancing retention for passive avoidance learning in mice. This test was used to select compounds with potential therapeutic properties for the treatment of cognitive disorders. Reference drugs that gave positive results in this procedure included d-amphetamine, magnesium pemoline, methyl phenidate, picrotoxin, phenytoin, and ethosuximide. All active compounds gave inverted U-shaped dose-response curves. The most active compounds of the 3-(aryloxy)pyridines included 3-phenoxypyridine (1), 3-(2-fluorophenoxy)pyridine (2), 3-(4-fluorophenoxy)pyridine (4), 3,3'-oxybis(pyridine) (23), and 3,3'-oxybis(pyridine) 1-oxide (24). 3-Phenoxypyridine (1) was clearly superior to all of the analogues tested in terms of the level of retention, grammometric potency, and the breadth of its inverted U-shaped dose-response curve. It was given the designation of CI-844 and after a detailed study of its pharmacological profile was submitted for preclinical toxicology.
Non-RCT
Animal Study3-(aryloxy)pyridines show potential in enhancing memory retention for cognitive disorders, with 3-phenoxypyridine (1) showing the most activity and potential for preclinical toxicology studies.
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