Synthesis and Biological Evaluation of 3,7-Diazabicyclo[4.3.0]nonan-8-ones as Potential Nootropic and Analgesic Drugs

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• 作者：Elisabetta Martini ; Lorenzo Di Cesare Mannelli ; Gianluca Bartolucci ; Carlo Bertucci ; Silvia Dei ; Carla Ghelardini ; Luca Guandalini ; Dina Manetti ; Serena Scapecchi ; Elisabetta Teodori ; Maria Novella Romanelli
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：April 14, 2011
• 年：2011
• 卷：54
• 期：7
• 页码：2512-2516
• 全文大小：797K
• 年卷期：v.54,no.7(April 14, 2011)
• ISSN：1520-4804

文摘

A series of cis and trans 3,7-diazabicyclo[4.3.0]nonan-8-ones has been synthesized and tested for their ability to revert scopolamine-induced amnesia in the mouse passive-avoidance test. The racemates of the most potent compounds 4 and 7 were separated and tested, but no enantioselectivity was found for the nootropic activity. Compounds 4 and 7 and their enantiomers displayed interesting antihyperalgesic activity in two models of neuropathic pain (streptozotocin-induced and oxalilplatin-induced neuropathy) in comparison with pregabalin.