Substituted (Pyrroloamino)pyridines:  Potential Agents for the Treatment of Alzheimer's Disease

A novel series of substituted (pyrroloamino)pyridines was synthesized, and the compounds were evaluated for cholinomimetic-like properties in vitro (inhibition of [3H]quinuclidinyl benzilate binding) and in vivo (reversal of scopolamine-induced dementia) as potential agents for the treatment of Alzh...

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Veröffentlicht in:Journal of medicinal chemistry 1996-01, Vol.39 (2), p.582-587
Hauptverfasser: Davis, Larry, Klein, Joseph T, Kapples, Kevin J, Huger, Francis P, Smith, Craig P, Petko, Wayne W, Cornfeldt, Michael, Effland, Richard C
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Sprache:eng
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Zusammenfassung:A novel series of substituted (pyrroloamino)pyridines was synthesized, and the compounds were evaluated for cholinomimetic-like properties in vitro (inhibition of [3H]quinuclidinyl benzilate binding) and in vivo (reversal of scopolamine-induced dementia) as potential agents for the treatment of Alzheimer's disease. Compounds displaying significant activity were more broadly evaluated, which revealed the presence of a desirable adrenergic component of activity. The synthesis and structure−activity relationships for this series is presented, along with the biological profiles of selected compounds.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm950644v