Acetylcholinesterase inhibition by fused dihydroquinazoline compounds

A new type of dihydroquinazoline-based inhibitor of acetylcholinesterase (AChE) is described. These compounds were designed to interact with the catalytic site of AChE in a manner similar to the known inhibitor tacrine. In a manner analogous to the potency enhancement obtained by addition of chlorin...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1996-03, Vol.6 (6), p.737-742
Main Authors: Jaén, Juan C., Gregor, Vlad E., Lee, Chet, Davis, Robert, Emmerling, Mark
Format: Article
Language:English
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Summary:A new type of dihydroquinazoline-based inhibitor of acetylcholinesterase (AChE) is described. These compounds were designed to interact with the catalytic site of AChE in a manner similar to the known inhibitor tacrine. In a manner analogous to the potency enhancement obtained by addition of chlorine atoms to the tacrine molecule, a 3-chloro derivative of the parent hexahydroazepino[2,1- b]quinazoline structure was found to be about 8 times more potent as an AChE inhibitor than the unsubstituted compound. A new type of dihydroquinazoline-based inhibitor of acetylcholinesterase (AChE) is described. These compounds have been designed to mimic the mode of interaction of the known inhibitor tacrine with AChE. The potency enhancement obtained by chlorine substitution on the benzene ring (compound 8) is similar to that observed for tacrine derivatives.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(96)00102-3