Syntesis and Amnesia-Reversal Activity of a Series of 7- and 5-Membered 3-Acylamino Lactams

Article abstract of DOI:10.1021/jm00063a001

A series of 3-(acylamino)-ε-caprolactams and 3-(acylamino)-2-pyrrolidinones was synthesized.Some of these compounds reversed at different degrees electroconvulsive shock- and Scopolamine-induced amnesia, using a step-through passive avoidance in mice.Classical nootropic drugs, i.e., Aniracetam, Oxiracetam, and Piracetam, were used as reference compounds.Within the analyses of data performed, we introduced a new parameter, the confrontation index (CI), which is a function of Mann-Whitney's U statistic.The CI permits a common scale of activity of substances to be generated, independently of probabilistic hypotheses, with higher scores representing higher activities.The most active compounds were characterized by the formylamino and <3-(trifluoromethyl)benzoyl>amino groups in the 3-position of the ring.None of the substances assayed showed any effect on spontaneous behavior and neurovegetative system.