L. Angelucci et al., SYNTHESIS AND AMNESIA-REVERSAL ACTIVITY OF A SERIES OF 7-MEMBERED AND5-MEMBERED 3-ACYLAMINO LACTAMS, Journal of medicinal chemistry, 36(11), 1993, pp. 1511-1528
A series of 3-(acylamino)-epsilon-caprolactams and 3-(acylamino)-2-pyr
rolidinones was synthesized. Some of these compounds reversed at diffe
rent degrees electroconvulsive shock- and Scopolamine-induced amnesia,
using a step-through passive avoidance in mice. Classical nootropic d
rugs, i.e., Aniracetam, Oxiracetam, and Piracetam, were used as refere
nce compounds. Within the analyses of data performed, we introduced a
new parameter, the confrontation index (CI), which is a function of Ma
nn-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 c
ompounds were characterized by the formylamino and [3-(trifluoromethyl
)benzoyl]amino groups in the 3-position of the ring. None of the subst
ances assayed showed any effect on spontaneous behavior and neuroveget
ative system.