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2-氧代-1-吡咯烷磺酸衍生物的合成及其益智活性

Synthesis and nootropic activity of 2-oxo-1-pyrrolidinesulfonic acid derivatives.

作者信息

Cerri A, Farina C, Pinza M, Banfi S

机构信息

Ist-Laboratori Per la Ricerca Biomedica (Milano), Italy.

出版信息

Farmaco. 1991 Jul-Aug;46(7-8):959-66.

PMID:1793478
Abstract

The synthesis of a series of 2-oxo-1-pyrrolidinesulfonic acid derivatives, as potential nootropic agents, is reported. Such compounds were designed to have chemical and physico-chemical properties intermediate between 2-oxo-1-pyrrolidineacetamides (e.g. oxiracetam) and 1-acyl-2-pyrrolidinones (e.g. aniracetam). The ability of these compounds to counteract the ECS-induced amnesia in mice was assessed in a one trial, step through, passive avoidance paradigm. Whilst oxiracetam and aniracetam confirmed their antiamnestic action, none of the title compounds showed a statistically significant activity.

摘要

报道了一系列作为潜在促智剂的2-氧代-1-吡咯烷磺酸衍生物的合成。设计这类化合物使其具有介于2-氧代-1-吡咯烷乙酰胺(如奥拉西坦)和1-酰基-2-吡咯烷酮(如阿尼西坦)之间的化学和物理化学性质。在单次试验、穿梭、被动回避范式中评估了这些化合物对抗小鼠电惊厥休克(ECS)诱导失忆的能力。虽然奥拉西坦和阿尼西坦证实了它们的抗失忆作用,但标题化合物均未表现出统计学上显著的活性。

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