Bioorganic and Medicinal Chemistry Letters p. 737 - 742 (1996)
Update date:2022-08-18
Topics:
Jaen, Juan C.
Gregor, Vlad E.
Lee, Chet
Davis, Robert
Emmerling, Mark
A new type of dihydroquinazoline-based inibitor 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.
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