Synthesis and amnesia-reversal activity of a series of 7-and 5-membered 3-acylamino lactams

L Angelucci, P Calvisi, R Catini… - Journal of medicinal …, 1993 - ACS Publications
L Angelucci, P Calvisi, R Catini, U Cosentino, R Cozzolino, P De Witt, O Ghirardi…
Journal of medicinal chemistry, 1993ACS Publications
A series of 3-(acylamino)-e-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, ie, Aniracetam, Oxiracetam, and Piracetam, were used as
reference compounds. Within the analyses of data performed, we introduced a new
parameter, the confrontation index (Cl), which is a function of Mann-Whitney's U statistic. The …
A series of 3-(acylamino)-e-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, ie, Aniracetam, Oxiracetam, and Piracetam, were used as reference compounds. Within the analyses of data performed, we introduced a new parameter, the confrontation index (Cl), which is a function of Mann-Whitney’s U statistic. The Cl 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-(trifluo-romethyl) benzoyl] amino groups in the 3-position of the ring. None of the substances assayed showed any effect on spontaneous behavior and neurovegetative system.
Over the last two decades, an ever growing interest has been devotedto the search for new drugs that might be useful for prevention or treatment of human cognitive disorders. Although cognitive impairments may occur in people of any age, the increase in life expectancy has made treatment of age-related cognitive disorders one of today’s scientific, medical, and social targets. Cognition enhancingagents include a wide range of
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