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1.
J Med Chem ; 36(11): 1511-9, 1993 May 28.
Article in English | MEDLINE | ID: mdl-8496921

ABSTRACT

A series of 3-(acylamino)-epsilon-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.


Subject(s)
Amnesia/drug therapy , Lactams/chemical synthesis , Psychotropic Drugs/chemical synthesis , Amnesia/etiology , Animals , Brain/enzymology , Cholinesterase Inhibitors/pharmacology , Drug Design , Electroshock , In Vitro Techniques , Lactams/pharmacology , Male , Mice , Psychotropic Drugs/pharmacology , Pyrrolidinones/chemical synthesis , Pyrrolidinones/pharmacology , Rats , Rats, Inbred F344 , Scopolamine , Structure-Activity Relationship
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