SYNTHESIS AND AMNESIA-REVERSAL ACTIVITY OF A SERIES OF 7-MEMBERED AND 5-MEMBERED 3-ACYLAMINO LACTAMS

被引:19
作者
ANGELUCCI, L
CALVISI, P
CATINI, R
COSENTINO, U
COZZOLINO, R
DEWITT, P
GHIRARDI, O
GIANNESSI, F
GIULIANI, A
GUARALDI, D
MISITI, D
RAMACCI, MT
SCOLASTICO, C
TINTI, MO
机构
[1] SIGMA TAU PHARMACEUT CO,1ST RIC SENESCENZA,VIA PONTINA KM 30400,I-00040 POMEZIA,ITALY
[2] UNIV ROMA LA SAPIENZA,DIPARTIMENTO STUDI CHIM & TECNOL SOSTANZE BIOLOGICAMENTE ATT,I-00185 ROME,ITALY
[3] CTR CNR STUDIO SOSTANZE ORGAN NAT,I-20133 MILAN,ITALY
[4] SIGMA TAU PHARMACEUT CO,DIPARTIMENTO RIC CHIM,I-00040 POMEZIA,ITALY
[5] UNIV ROMA LA SAPIENZA,1ST FARMACOL 2,I-00185 ROME,ITALY
[6] UNIV MILAN,DIPARTIMENTO CHIM FIS & ELETTROCHIM,I-20133 MILAN,ITALY
关键词
D O I
10.1021/jm00063a001
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:1511 / 1528
页数:18
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