SYNTHESIS AND AMNESIA-REVERSAL ACTIVITY OF A SERIES OF 7-MEMBERED AND5-MEMBERED 3-ACYLAMINO LACTAMS

Citation
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
Citations number
35
Categorie Soggetti
Chemistry Medicinal
ISSN journal
00222623
Volume
36
Issue
11
Year of publication
1993
Pages
1511 - 1528
Database
ISI
SICI code
0022-2623(1993)36:11<1511:SAAAOA>2.0.ZU;2-R
Abstract
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.