Design, synthesis, and preliminary pharmacological evaluation of 1,4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents

被引：35

作者：

Manetti, D

Ghelardini, C

Bartolini, A

Bellucci, C

Dei, S

Galeotti, N

Gualtieri, F

Romanelli, MN

Scapecchi, S

Teodori, E

机构：

[1] Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy

[2] Univ Florence, Dipartimento Farmacol Preclin & Clin, I-50139 Florence, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2000年 / 43卷 / 10期

关键词：

D O I：

10.1021/jm991170t

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several 4-substituted 1,4-diazabicyclo[4.3.0]nonan-9-ones have been synthesized and tested in vivo on mouse passive avoidance test, to evaluate their nootropic activity. The results show that they represent a new class of nootropic drugs with a pharmacological profile very similar to that of piracetam, showing much higher potency with respect to the reference. Among the compounds studied, 7 (DM 232) shows outstanding potency, being active at the dose of 0.001 mg kg(-1) sc.

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页码：1969 / 1974

页数：6

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