Design, synthesis and molecular modeling of 3-acylamino-2- Carboxyindole NMDA receptor glycine-site antagonists

Abstract The syntheses and molecular modeling of several 3-acylamino-2-carboxyindole antagonists of the glycine binding site associated with the NMDA receptor complex is described. Tertiary amide 8 is a potent antagonist; this result is rationalized by a preferred cis amide bond conformation. The potency of the trans secondary oxalamide 10 is explained by binding to the receptor in its enolic form.