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.

Synthesis and Biological Evaluation of 3,7-Diazabicyclo[4.3.0]2 nonan-8-ones as Potential Nootropic and Analgesic Drugs / E. Martini; L. Di Cesare Mannelli; G. Bartolucci; C. Bertucci; S. Dei; C. Ghelardini; L. Guandalini; D. Manetti; S. Scapecchi; E. Teodori; M. N. Romanelli. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 54:(2011), pp. 2512-2516. [10.1021/jm101376k]

Synthesis and Biological Evaluation of 3,7-Diazabicyclo[4.3.0]2 nonan-8-ones as Potential Nootropic and Analgesic Drugs

MARTINI, ELISABETTA;DI CESARE MANNELLI, LORENZO;BARTOLUCCI, GIAN LUCA;DEI, SILVIA;GHELARDINI, CARLA;GUANDALINI, LUCA;MANETTI, DINA;SCAPECCHI, SERENA;TEODORI, ELISABETTA;ROMANELLI, MARIA NOVELLA
2011

Abstract

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.
2011
54
2512
2516
E. Martini; L. Di Cesare Mannelli; G. Bartolucci; C. Bertucci; S. Dei; C. Ghelardini; L. Guandalini; D. Manetti; S. Scapecchi; E. Teodori; M. N. Romanelli
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/539458
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