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新型 sunifiram 和 sapunifiram 类似物的设计、合成及促智活性研究,这两种化合物均为强效认知增强剂。

Design, synthesis and nootropic activity of new analogues of sunifiram and sapunifiram, two potent cognition-enhancers.

机构信息

Department of Pharmaceutical Sciences, Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles (HeteroBioLab), University of Florence, 50019 Sesto Fiorentino, Italy.

出版信息

Bioorg Med Chem. 2009 Nov 1;17(21):7606-14. doi: 10.1016/j.bmc.2009.08.055. Epub 2009 Sep 3.

Abstract

A series of amides and sulfonamides, structurally related to DM235 (sunifiram) and MN19 (sapunifiram), derived by ring expansion or contraction, or by inversion of the exocyclic amide function, have been synthesized and tested for cognition-enhancing activity in the mouse passive-avoidance test. Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, and with a potency similar to the parent compounds.

摘要

一系列酰胺和磺酰胺,通过环的扩张或收缩,或通过对外环酰胺官能团的反转,与 DM235(噻奈普汀)和 MN19(沙宾福林)结构相关,已经被合成并在小鼠被动回避测试中测试了其认知增强活性。一些化合物显示出良好的抗遗忘和促认知活性,其效力高于吡拉西坦,与母体化合物的效力相似。

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