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Acetylcholinesterase inhibition by fused dihydroquinazoline compounds

1996; Elsevier BV; Volume: 6; Issue: 6 Linguagem: Inglês

10.1016/0960-894x(96)00102-3

1464-3405

Juan C. Jaén, V. Gregor, Chet Lee, Robert E. Davis, Mark R. Emmerling,

Quinazolinone synthesis and applications

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.